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ANTIBIOTICS

(1) sulfonamides
--indicated for urinary tract infections, cystitis (bladder inflammation)
--Bactrim DS - sulfamethoxazole/trimethoprim
--crystalluria
--patient counseling for sulfonamides:
--drink plenty of water
--avoid ultraviolet radiation
--phototoxic reactions
--finish medication
(2) nitrofurantoin
--Macrodantin, Macrobid
--indicated for urinary tract infections, cystitis
--patient counseling:
--take with food
--urine discoloration
--finish medication
phenazopyridine - sometimes prescribed with sulfonamides and nitrofurantoin
--not an antibiotic
--reddish dye that exerts local anesthetic effect on urinary tract mucosa
--Pyridium Rx 100 mg, 200 mg
--Azo-Standard OTC 95 mg
--patient counseling
--drink plenty of water
--urine discoloration
(3) penicillins (penicillin, ampicillin, amoxicillin)
--patient counseling:
--penicillin, ampicillin
--take on empty stomach
--amoxicillin can be taken without regard to meals
--finish medication
(4) tetracyclines (tetracycline, minocycline, doxycycline)
--doxycycline 20 mg (Periostat)
--indicated for periodontitis (collagenase)
--gingivitis (plaque)
--chlorhexidine (Peridex)
--patient counseling for tetracyclines:
--do not take with divalent/trivalent cations
--chelation (calcium, aluminum, magnesium, iron, zinc)
--phototoxic reactions
--finish medication
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(5) fluoroquinolones
--ciprofloxacin
--moxifloxacin (Avelox)

levofloxacin (Levaquin)
gemifloxacin (Factive)

--patient counseling for fluoroquinolones:


--chelation
--phototoxic reactions
--Black Box Warning:
--Achilles or other tendon rupture
--finish medication
ophthalmic fluoroquinolones
--indicated for bacterial conjunctivitis (pink eye)
--gatifloxacin (Zymaxid)
--ofloxacin (Ocuflox)
--ciprofloxacin (Ciloxan)
--besifloxacin (Besivance)
--moxifloxacin
--Vigamox (0.5%)
`
--dosing interval - three times daily
--Moxeza (0.5%)
--dosing interval - twice daily
(6) cephalosporins
--1st generation
--cefadroxil, cephalexin (Keflex)
--2nd generation
--cefaclor, cefprozil (Cefzil), cefuroxime (Ceftin)
--3rd generation
--cefdinir, cefpodoxime, cefditoren (Spectracef), cefixime (Suprax)
--patient counseling:
--cefdinir
--avoid antacids (chelation)
--red stool
--do not refrigerate oral suspension
--cefditoren
--take with food
--finish medication

(7) macrolides
--erythromycin, clarithromycin (Biaxin), azithromycin
--azithromycin available in 3 trade names Zithromax, Z-Max, AzaSite
--Zithromax
--tablet (250 mg, 500 mg)
--powder for oral suspension:
--100 mg/5 mL, 200 mg/5 mL
--reconstituted in pharmacy
--1 gram single dose powder packet
--indicated for Chlamydia
--Z-Max
--extended-release microspheres for oral suspension
--2 gram single dose bottle
--AzaSite:
--1% azithromycin ophthalmic solution
--indicated for bacterial conjunctivitis
--patient counseling for macrolides:
--erythromycin, clarithromycin
--take with food
--azithromycin
--avoid antacids (chelation)
--Z-Max
--take on empty stomach
--AzaSite
--refrigerate in pharmacy
(8) lincosamides
--clindamycin
--capsule (150 mg, 300 mg) Cleocin
--granules for oral solution (75 mg/5 mL) Cleocin
--vaginal cream (Cleocin Vaginal Cream 2%)
--indicated for bacterial vaginosis
--vaginal suppository (Cleocin Ovules 100 mg)
--indicated for bacterial vaginosis
--topical dosage form (Cleocin T 1%)
--indicated for acne
--patient counseling:
--granules for oral solution store at room temperature after reconstitution
--oral dosage forms black stool
--finish medication
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(9) nitroimidazoles
--metronidazole
--effective against protozoa and bacteria
--administered orally, vaginally, topically
--oral metronidazole (Flagyl)
--indicated for trichomoniasis
--Trichomonas vaginalis
--female symptomatic
--male asymptomatic
--treat both partners
--250 mg, 500 mg tablets, 375 mg capsule
--dose/dosing interval for trichomoniasis
--250 mg TID for 7 days or 2 gram single dose
--vaginal metronidazole (MetroGel-Vaginal, Vandazole Vaginal)
--indicated for bacterial vaginosis
--0.75% gel
--one applicatorful vaginally at bedtime for 5 days
--topical metronidazole - indicated for rosacea
--patient counseling
--do not drink alcoholic beverages.
--disulfiram-like reaction
--avoid alcohol for 3 days after discontinuing metronidazole
--finish medication
(10) oxazolidinones
linezolid (Zyvox)
(11) antituberculosis agent
--rifampin (Rifadin)
--indicated for tuberculosis
--use in combination with isoniazid and pyrazinamide
--patient counseling:
--discolors body secretions
--decreases effectiveness of hormonal contraceptives
--take on empty stomach
Xifaxanrifaximin
--indicated for Travelers Diarrhea cause by E. Coli
--therapeutic category - antibiotic

BISPHOSPHONATES
--indicated for osteoporosis, Paget's Disease of the bone, corticosteroid induced osteoporosis
osteoporosis - decrease in bone density caused by bone resorption
--osteoblast, osteoclast
--bisphosphonates decrease bone resorption
Pagets Disease of the bone
--clinical term - osteitis deformans
--episodes of increased bone resorption followed by excessive attempts at repair
--repaired bone is weak (individuals over 50)
corticosteroid induced osteoporosis
--corticosteroids inhibit osteoblasts and increase bone resorption
--bisphosphonates are indicated in patients taking more than 7.5 mg prednisone daily
Bisphosphonates:
--risedronate (Actonel, Atelvia)
Actonel IR tablet
--35 mg tablet once weekly
--150 mg tablet once monthly
Atelvia - enteric coated tablet
-- 35 mg once weekly
--alendronate ( Fosamax)
--70 mg tablet
--70 mg/75 mL oral solution
--once weekly
--Fosamax Plus D two products available
--70 mg alendronate, 70 mcg of cholecalciferol
--70 mg alendronate, 140 mcg of cholecalciferol
--once weekly
--cholecalciferol - clinical term for Vitamin D
--70 mcg of cholecalciferol = 2,800 units of Vit D
--140 mcg = 5,600 units
--ibandronate (Boniva)
--150 mg tablet
--once a month
--parenteral (IV)
--every 3 months
--zoledronic acid (Reclast)
--parenteral (IV)
--once a year
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Patient counseling for oral bisphosphonates:


1.
for all except Ateliva
--take on empty stomach 30 minutes before breakfast
--Atelvia take immediately after breakfast
2.
for all - take with a full glass of water
3.
for all - remain upright for 30 minutes after administration
Two other parenteral medications for osteoporosis - not bisphosphonates
--teriparatide (Forteo)
--therapeutic category - parathyroid hormone (PTH) analog
--subcutaneous injection
--once daily
--must be refrigerated at all times
--denosumab (Prolia)
--therapeutic category monoclonal antibody
--indicated in patients with a high risk of fractures
--subcutaneous injection
--every 6 months
SERMS - SELECTIVE ESTROGEN RECEPTOR MODULATORS
--estrogen receptor agonists, estrogen receptor antagonists
--activate estrogenic pathways in some tissues (agonist)
--block estrogenic pathways in others (antagonist)
tamoxifen
--indicated for breast cancer prophylaxis in high risk women
toremifene (Fareston)
--indicated for breast cancer prophylaxis in high risk women
raloxifene (Evista)
--indicated for breast cancer prophylaxis, osteoporosis
ospemifene (Osphena)
--indicated for vaginal atrophy, dyspareunia
--vaginal atrophy (clinical term atrophic vaginitis)
--painful intercourse (clinical term - dyspareunia)
conjugated estrogens/bazedoxifene (Duavee)
--indicated for vasomotor symptoms, osteoporosis
--vasomotor symptoms (hot flashes)
--bazedoxifene is a SERM
--reduce endometrial hyperplasia (endometrium)

WEIGHT LOSS
Obesity medical condition in which excess body fat may have an adverse effect on health.
--obese if BMI 30 or above
phentermine (anorexiant) - CIV
--37.5 mg capsule and tablet (Adipex P)
--15 mg, 30 mg, 37.5 mg ODT (Suprenza)
--sympathomimetic (satiety center)
--indicated for short-term weight management
diethylpropion (anorexiant) - CIV
--25 mg tablet, 75 mg ER tablet
--sympathomimetic
--indicated for short-term weight management
lorcaserin (anorexiant) - CIV
--10 mg tablet (Belviq)
--indicated for chronic weight management
bupropion, naltrexone (anorexiant)
--90 mg, 8 mg (Contrave)
--indicated for chronic weight management
--bupropion - aminoketone antidepressant
--naltrexone - opioid antagonist
--mesolimbic dopamine circuit (i.e. reward system)
orlistat (lipase inhibitor)
--60 mg capsule (Alli) - OTC 120 mg capsule (Xenical) Rx
--inhibits gastrointestinal lipase enzymes (bothersome adverse effects - psyllium)
--indicated for chronic weight management
phentermine/topiramate Qsymia (anorexiant) - CIV
--sympathomimetic, anticonvulsant
--initial dose/dosing interval - 3.75 mg phentermine/23 mg topiramate for 2 weeks
--increase to 7.5 mg/46 mg for 12 weeks
--increase to 11.25 mg/69 mg for 2 weeks (prn)
--increase to 15 mg /92 mg strength for 12 weeks
--available through REMS - Risk Evaluation and Mitigation Strategies
--indicated for chronic weight management
liraglutide - Saxenda
--appetite suppressant
--subcutaneous injection
--initial dose 0.6 mg (titrate dose)
--maintenance dose 3 mg
--indicated for chronic weight management
7

ANTIDIABETICS
Diabetes Mellitus - disorder characterized by hyperglycemia resulting from a lack of insulin
and/or insulin resistance.
Two Types:
Type 1, Type 2
Type 1 patients must use insulin
Regular R
--classified as rapid-acting
--onset of action ~30 minutes
--duration of action - ~8 hours
--Humulin R, Novolin R
--OTC
NPH Neutral Protamine Hagedorn
--classified as intermediate-acting (isophane insulin)
--onset ~1 hour
--duration - between 12 - 16 hours
--Humulin N, Novolin N
--OTC
Humulin 70/30
Novolin 70/30
--70% NPH, 30% Regular
--onset - ~30 minutes
--duration - between 12 - 16 hours
--OTC
Insulin Analogs
--rapid-acting insulin analogs
--very fast onset
--long-acting insulin analogs
--slow onset
--basal insulin level
Rapid-acting insulin analogs:
Humalog insulin lispro
Novolog insulin aspart
Apidra insulin glulisine
--onset - ~15 minutes
--duration ~3 hours
--used in combination with long-acting insulin analogs
--Rx

Rapid-acting insulin analog combination products:


Humalog Mix 75/25
--75% insulin lispro protamine, 25% insulin lispro
--two absorption phases
--onset ~15 minutes
--duration of action - ~18 hours
--Rx
Novolog Mix 70/30
--70% insulin aspart protamine, 30% insulin aspart
--onset ~15 minutes
--duration of action - ~18 hours
--Rx
Long-acting insulin analogs:
Lantus insulin glargine
Toujeo - insulin glargine
Levemir insulin detemir
Tresiba - insulin degludec
--onset ~1 hour
--duration ~24 hours
--Rx
Insulin is dosed in units
--100 Units of insulin/mL of solution
--exceptions:
--Humulin R U-500 (500 units/mL)
--patients requiring more than 200 units of insulin daily
--Toujeo (insulin glargine) (300 units/mL)
--Humalog U-200 (200 units/mL)
--Tresiba - 100 units/mL, 200 units/mL
Oral antidiabetics
Sulfonylureas
--stimulate insulin secretion and increase tissue sensitivity to insulin
--severe hypoglycemia in OD
--alcohol may cause hypoglycemia
--chlorpropamide
--glipizide (Glucotrol, Glucotrol XL)
--glimepiride (Amaryl)
--glyburide (Glynase Prestab)
Meglitinides
--stimulate insulin secretion (hypoglycemia in OD)
--alcohol may cause hypoglycemia
--Starlix (nateglinide), Prandin (repaglinide)
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Biguanides
--increase tissue sensitivity to insulin
--metformin (Glucophage, Glucophage XR, Fortamet, Glumetza)
--BBW
--cyanocobalamin
Thiazolidinediones
--increase tissue sensitivity to insulin
--Actos pioglitazone
--Avandia rosiglitazone
--BBW
Alpha-glucosidase inhibitors
--delay digestion of ingested carbohydrates
--Precose (acarbose)
--Glyset (miglitol)
--take with first bite of each main meal
Incretin Mimetics
exenatide
--Byetta
--administer 1 hour before breakfast and supper
--subcutaneous injection (5 mcg, 10 mcg)
--two separate pre-filled, multidose injection pens
--Bydureon (extended-release exenatide injection suspension)
--once weekly
--subcutaneous injection (2 mg)
--exenatide powder reconstituted
--one single dose injection pen
liraglutide - Victoza
--once daily
--subcutaneous injection (0.6 mg, 1.2 mg, 1.8 mg)
--one pre-filled, multidose injection pen
albiglutide - Tanzeum
--once weekly
--subcutaneous injection (30 mg, 50 mg)
--albiglutide powder reconstituted
--two separate, single dose injection pens
dulaglutide - Trulicity
--once weekly
--subcutaneous injection (0.75mg, 1.5 mg)
--two separate pre-filled, single dose injection pens
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Dipeptidyl Peptidase 4 Inhibitors


--DPP-4 is an enzyme that metabolizes incretin hormones
--Januvia (sitagliptin)
Onglyza (saxagliptin)
--Tradjenta (linagliptin)
Nesina (alogliptin)
Dipeptidyl Peptidase 4 Inhibitor Combination Products
--Janumet (sitagliptin, metformin)
--Jentadueto (linagliptin, metformin)
--BBW
Sodium-Glucose Co-Transporter 2 (SGLT2) Inhibitors
--block reabsorption of glucose by the kidney
--glucose excreted in the urine
--Invokana (canagliflozin)
--once daily 30 minutes before breakfast
--Invokamet (canagliflozin, metformin)
--twice daily with meals
--BBW
--Farxiga (dapagliflozin)
--once daily in the morning without regard to meals
--Xigduo (dapagliflozin, metformin)
--once daily in the morning with breakfast
--BBW
--Jardiance (empagliflozin)
--once daily in the morning without regard to meals
--Glyxambi (empagliflozin, linagliptin)
--once daily in the morning without regard to meals
Combination Antidiabetics
Glucovance (glyburide, metformin)
Kombiglyze XR (saxagliptin, metformin)
Invokamet (canagliflozin, metformin)
Kazano (alogliptin, metformin)
ActoPlus Met (pioglitazone, metformin)
Avandamet (rosiglitazone, metformin)
Duetact (pioglitazone, glimepiride)

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DERMATITIS

General symptoms:
--blisters (vesicles) itching (pruritus)
redness (erythema)
--bleeding
crusting
dry skin (xeroderma)
Types:
1. atopic dermatitis (eczema)
--scalp, head, inside of elbows and knees
--treatment:
--moisturizers
--topical corticosteroids
--topical immunosuppressants
--pimecrolimus (Elidel), tacrolimus (Protopic)
--calcineurin inhibitors
--BBW's - skin cancer, don't use in children under 2 years
--oral immunosuppressants (methotrexate) - severe cases only
2. contact dermatitis (irritant, allergic)
3. seborrheic dermatitis
--scalp [newborns (cradle cap), adults (dandruff)]
ACNE
--acne vulgaris
--inflammatory disorder of the pilosebaceous unit (hair follicle/sebaceous gland)
--sebum, comedone, Propionibacterium acnes (P acnes)
--inflammatory lesions (papule, pustule, nodule)
Treatment:
--Mild Acne (minimal inflammation, minimal papules)
--benzoyl peroxide
--active against Propionibacterium acnes
--exfoliant
--Moderate Acne (moderate inflammation with papule/pustule formation)
--topical antibiotics - clindamycin (Cleocin T), erythromycin, azelaic acid (Azelex
--active against Propionibacterium acnes
--topical retinoids
--therapeutic category - antiacne
--antiacne class - retinoid (derivatives of Vitamin A)
--increase epidermal cell turnover (decreases comedone formation)
--tretinoin (Retin-A), adapalene (Differin), tazarotene (Tazorac)
--oral antibiotics
--doxycycline (Vibramycin, Doryx, Oracea), minocycline (Minocin)
--active against Propionibacterium acnes
--oral contraceptives - norgestimate, norethindrone, drospirenone
--Severe Acne (severe inflammation, deep nodules leading to scarring)
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trade names: Claravis, Absorica

ISOTRETINOIN

therapeutic category - antiacne (retinoid)


--reduces sebum production
--twice daily
BBW - do not take during pregnancy - teratogen (teratogenic substance)
--iPLEDGE
--program to reduce birth defects
patient counseling:
avoid in pregnancy
blood donations
epistaxis

take with food


phototoxic reactions
hypertriglyceridemia cheilitis
xeroderma

ROSACEA
--skin condition characterized by redness, dilated blood vessels, papules, pustules
--symptoms:
--flushing, erythema, papules, pustules, dilated blood vessels, rhinophyma
--triggers:
--sun exposure, hot/cold weather, wind, stress
--treatment:
--topical metronidazole (nitroimidazole)
--MetroLotion, MetroCream
--Azelex (azelaic acid) - antiacne agent
--Mirvaso (brimonidine) - anti-inflammatory
--Soolantra (ivermectin) - antiparasitic agent
PSORIASIS
--non-contagious, chronic, relapsing/remitting, autoimmune disease
--T cells
--increased skin cell proliferation
--plaque psoriasis - inflamed skin covered by red/silvery scales (plaque)
--psoriatic arthritis
Treatment:
--calcipotriene (Dovonex)
--Vitamin D analog - decreases cell proliferation
--topical corticosteroids
--anti-inflammatory, immunosuppressive, antipruritic
--ranked by potency based on ability to cause vasoconstriction
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Very High Potency


--betamethasone dipropionate (Diprolene AF)
--augmented formulation - propylene glycol
--clobetasol (Temovate)
halobetasol (Ultravate)
High Potency
--amcinonide
halcinonide (Halog)
--fluocinonide
desoximetasone (Topicort)
--betamethasone dipropionate - non augmented
Medium Potency
--triamcinolone
mometasone (Elocon)
--fluticasone (Cutivate)
fluocinolone (Synalar)
--hydrocortisone butyrate (Locoid) hydrocortisone valerate (Westcort)
Low Potency
--alclometasone (Aclovate)
--hydrocortisone
--desonide (DesOwen)
--low potency preferred on face, groin, axilla
--oral medications:
--methotrexate (psoriatic arthritis)
--apremilast (Otezla)
--psoriatic arthritis
--phosphodiesterase-4 inhibitor
ANTICOAGULANTS
indicated for thrombosis (thrombus - clinical term for blood clot)
Vitamin K Antagonist
--warfarin (Coumadin)
--inhibits synthesis of vitamin K dependent clotting factors (II, VII, IX, X)
--once daily
--vitamin K reduces Coumadin's effectiveness
--green leafy vegetables, multiple vitamins
--vitamin K tablets (phytonadione Mephyton)
Thrombin Inhibitor
--dabigatran (Pradaxa)
--twice daily
--original container
--Praxbind
Factor Xa Inhibitors
--rivaroxaban (Xarelto)
--once daily
--apixaban (Eliquis)
--twice daily
--edoxaban (Savaysa)
--once daily
--fondaparinux (Arixtra)
14

ANTIPLATELET AGENTS
prasugrel (Effient)
cilostazol
--cilostazol also indicated for intermittent claudication
--periodic leg pain (claudication clinical term for lameness)
clopidogrel (Plavix)
--BBW - decreased effectiveness in poor metabolizers
--drug interaction with proton pump inhibitors - decrease metabolite formation
--omeprazole (Prilosec)
esomeprazole (Nexium)
--lansoprazole (Prevacid)
rabeprazole (Aciphex)
--pantoprazole(Protonix)
dexlansoprazole (Dexilant)
Aggrenox (aspirin, dipyridamole)
--variable release capsule
--25 mg IR aspirin, 200 mg ER dipyridamole
ticagrelor (Brilinta)
vorapaxar (Zontivity)
Patient counseling for antiplatelet agents:
--may cause bleeding
ALPHA 1- ADRENERGIC BLOCKING AGENTS
prazosin (Minipress)
terazosin
doxazosin (Cardura)
tamsulosin (Flomax)
alfuzosin (Uroxatral)
silodosin (Rapaflo)
--terazosin/doxazosin
--indicated for hypertension and BPH symptoms
--benign prostatic hyperplasia
--do not reduce prostate size
--5 - alpha reductase inhibitors reduce prostate size
--Avodart (dutasteride)
--Proscar (finasteride 5 mg)
--prevent conversion of testosterone to dihydrotestosterone
--Propecia (finasteride 1 mg) - indicated for alopecia
--prazosin - indicated for hypertension
--tamsulosin, silodosin, alfuzosin
--indicated for BPH symptoms (do not reduce prostate size)
Jalyn (dutasteride, tamsulosin) - improves outflow and decreases prostate size
patient counseling for alpha-1-adrenergic blocking agents:
--may cause syncope
15

IMPOTENCE

yohimbine (Yocon, Erex)


Caverject (alprostadil)
--therapeutic categories: prostaglandin, impotence agent, vasodilator
--powder for solution for intracavernosal injection
--reconstitute with bacteriostatic water for injection
--20 mcg, 40 mcg - following reconstitution use within 24 hours
--duration of action ~1 hour (over four hours - priapism)
--detumescence
MUSE (alprostadil) - Medicated Urethral System for Erection
--urethral suppository (bougie)
--duration of action ~1 hour
--125 mcg, 250 mcg, 500 mcg, 1000 mcg strengths
--once daily
Phosphodiesterase -5 Inhibitors
--Viagrasildenafil
Levitravardenafil
--Staxyn vardenafil
Stendra avanafil
Cialistadalafil
--MOA:
--nitric oxide is released in men when sexually aroused
--nitric oxide activates the enzyme guanylate cyclase
--this increases synthesis of cyclic guanosine monophosphate (cGMP)
--cGMP relaxes smooth muscle in the penis
--cGMP is metabolized by the enzyme phosphodiesterase - 5
Patient counseling for Viagra, Levitra, Staxyn, Stendra
--take 1 hour prior to sexual activity (four hour window of efficacy)
--Viagra/Levitra - empty stomach
--Staxyn, Stendra without regard to meals
Patient counseling for Cialis:
--take without regard to meals , 36 hour window of efficacy
Adverse effects with all phosphodiesterase -5 inhibitors:
--headache, flushing, blurred and/or altered color vision
Drug interactions with phosphodiesterase -5 inhibitors:
--nitrates (nitroglycerin, isosorbide), alpha -1 adrenergic blocking agents
Addyi - flibanserin
--HSDD in women
--serotonin agonist/antagonist (increases libido
--once daily
--hypotension

16

MIGRAINE HEADACHE

contraindicated:
--uncontrolled hypertension, ischemic heart disease
--ischemia clinical term for lack of blood to an area (angina pectoris)
sumatriptan (Imitrex)
--tablet (25 mg, 50 mg, 100 mg)
--1 at onset may repeat every 2 hours up to maximum daily dose (200 mg)
--nasal spray (20 mg)
--one spray at onset - may repeat once in 2 hours (max daily dose 40 mg)
--parenteral (subcutaneous injection)
--three trade names/two delivery systems
--Imitrex Injection (4 mg/0.5 mL, 6 mg/0.5 mL)
--Alsuma Injection (6 mg/0.5 mL)
--one injection at onset may repeat in 1 hour if needed
--maximum of 2 injections in 24 hours (1 hour between injections)
--Sumavel DosePro (6 mg/0.5 mL)
--high pressure nitrogen gas
--one injection at onset repeat in 1 hour if needed
--maximum of 2 injections in 24 hours (1 hour between injections)
--Treximet (85 mg sumatriptan, 500 mg naproxen)
--one tablet at onset repeat once in 2 hours if needed (max 24 hour dose 2 tablets)
zolmitriptan (Zomig)
--tablet (2.5 mg, 5 mg), ODT (2.5 mg, 5 mg) Zomig-ZMT
--1 at onset - may repeat every 2 hours up to maximum daily dose (10 mg)
naratriptan (Amerge)
rizatriptan (Maxalt)
--tablet (5 mg, 10 mg), ODT (5 mg, 10 mg) Maxalt MLT
--1 at onset, may repeat every 2 hours up to maximum daily dose (30 mg)
almotriptan (Axert)
frovatriptan (Frova)
eletriptan (Relpax)
--tablet (20, 40 mg)
--1 at onset may repeat every 2 hours up to maximum daily dose (80 mg)

17

I.

ORAL INHALERS
A.

Bronchodilators
1.
Metered Dose Inhalers (MDIs)
a.
albuterol - Proventil HFA, Ventolin HFA, ProAir HFA
b.
levalbuterol - Xopenex HFA
c.
ipratropium - Atrovent HFA
d.
olodaterol - Striverdi Respimat
e.
tiotropium - Spiriva Respimat
2.

B.

Corticosteroids
1.
Metered Dose Inhalers (MDIs)
a.
beclomethasone - QVAR
b.
fluticasone - Flovent HFA
c.
ciclesonide - Alvesco
2.

C.

Dry Powder Inhalers (DPIs)


a.
budesonide - Pulmicort Flexhaler
b.
mometasone - Asmanex Twisthaler
c.
fluticasone - Arnuity Ellipta

Combination Products
1.
Metered Dose Inhalers (MDIs)
a.
budesonide, formoterol - Symbicort
b.
mometasone, formoterol - Dulera
c.
fluticasone, salmeterol - Advair HFA
d.
ipratropium, albuterol Combivent Respimat
e.
tiotropium, olodaterol - Stiolto Respimat
2.

D.

Dry Powder Inhalers (DPIs)


a.
salmeterol - Serevent Diskus
b.
formoterol - Foradil Aerolizer
c.
tiotropium - Spiriva HandiHaler
d.
aclidinium Tudorza Pressair
e.
indacaterol Arcapta NeoHaler
f.
umeclidinium - Incruse Ellipta
g.
albuterol - ProAir Respiclick
h.
glycopyrrolate - Seebri Neohaler

Dry Powder Inhaler (DPI's)


a.
fluticasone, salmeterol - Advair Diskus
b.
fluticasone, vilanterol - Breo Ellipta
c.
umeclidinium, vilanterol - Anoro Ellipta
d.
glycopyrrolate, indacaterol - Utibron Neohaler

Antiviral Agent
1.
Dry Powder Inhaler (DPI)
a.
zanamivir Relenza

18

II.

INTRANASAL INHALERS
A.

Corticosteroids
1.
Nasal Sprays
a.
beclomethasone - Beconase AQ, Qnasl
b.
triamcinolone - Nasacort AQ
c.
budesonide - Rhinocort Aqua
d.
flunisolide
e.
fluticasone propionate - Flonase
f.
fluticasone furoate - Veramyst
g.
mometasone - Nasonex
h.
ciclesonide - Omnaris

B.

Mast Cell Stabilizers


1.
Nasal Spray
a.
cromolyn - Nasalcrom

C.

Pituitary Hormones
1.
Nasal Spray
a.
desmopressin acetate - DDAVP, Stimate

D.

Anticholinergics
1.
Nasal Spray
a.
ipratropium - Atrovent Nasal Spray

E.

Antihistamines
1.
Nasal Spray
a.
azelastine Astelin, Astepro

F.

Combination Product
1.
Nasal Spray
a.
azelastine, fluticasone - Dymista

G.

Medications for Osteoporosis


1.
Nasal Spray
a.
calcitonin - Miacalcin, Fortical

19

ORAL INHALERS
MDI's - metered dose inhalers (hydrofluoroalkane - HFA)
DPIs--dry powder inhalers
Bronchodilators and corticosteroids have two main indications:
--asthma, COPD (chronic obstructive pulmonary disease)
--asthma - inflammatory disease of the airways caused by inflammatory mediators
--histamine, leukotrienes, prostaglandins
--COPD - airway inflammation caused by smoking
--emphysema, alveoli
Bronchodilators
--do not treat underlying cause of asthma and COPD
--Sympathomimetic Bronchodilators (beta-2 agonists), Anticholinergic Bronchodilators
Two types of sympathomimetic bronchodilators:
Quick Relief Agents
--rescue inhalers
Long Term Control Agents
--asthma prophylaxis, maintenance treatment of COPD
Quick Relief Sympathomimetic Bronchodilators:
--albuterol (Proventil HFA, Ventolin HFA, ProAir HFA, ProAir Respiclick)
--levalbuterol (Xopenex HFA)
Long Term Control Sympathomimetic Bronchodilators:
--salmeterol (Serevent Diskus)
formoterol (Foradil Aerolizer)
--indacaterol (Arcapta NeoHaler)
olodaterol (Striverdi Respimat)
Long Term Control Sympathomimetics BBW: increase risk of asthma-related death
Anticholinergic Bronchodilators
--asthma prophylaxis, maintenance treatment of COPD
--ipratropium (Atrovent HFA)
--tiotropium (Spiriva HandiHaler)
--tiotropium (Spiriva Respimat)
--aclidinium (Tudorza Pressair)
--umeclidinium (Incruse Ellipta)
--glycopyrrolate (Seebri Neohaler)
Sympathomimetic/Anticholinergic Combination Products
--albuterol, ipratropium (Combivent Respimat)
--umeclidinium, vilanterol (Anoro Ellipta)
--tiotropium, olodaterol (Stiolto Respimat)
--glycopyrrolate, indacaterol (Utibron Neohaler)
20

Oral Corticosteroid Inhalers


--treat underlying cause of asthma and COPD
--asthma prophylaxis, maintenance treatment of COPD
--beclomethasone (QVAR)
--fluticasone (Flovent HFA, Arnuity Ellipta)
--budesonide (Pulmicort Flexhaler)
--mometasone (Asmanex Twisthaler)
--ciclesonide (Alvesco)
--oral candidiasis - thrush (candida albicans)
--gentian violet (topical antiseptic)
--nystatin suspension (antifungal)
--clotrimazole troches (imidazole antifungal)
Bronchodilator/Corticosteroid Combination Products
--asthma prophylaxis, maintenance treatment of COPD
--budesonide, formoterol (Symbicort)
--mometasone, formoterol (Dulera)
--fluticasone, salmeterol (Advair HFA, Advair Diskus)
--fluticasone, vilanterol (Breo Ellipta)
Antiviral Agent
--zanamivir (Relenza Diskhaler)
--neuraminidase inhibitor (Tamiflu - oseltamivir)
--zanamivir powder is contained in 5 mg blisters
--treatment of influenza - 10 mg BID for 5 days
--prevention of influenza in household setting - 10 mg once daily for 10 days
--prevention of influenza in community outbreak - 10 mg once daily for 28 days
Expiration Date of Inhalers (when removed from protective packaging)
--Advair Diskus (DPI) - one month
--Serevent Diskus (DPI) - 42 days
--Asmanex Twisthaler (DPI) - 45 days
--Anoro and Breo Ellipta (DPI) - 42 days
--ProAir Respiclick - 13 months
--Symbicort (MDI) - 3 months
--Ventolin HFA (MDI) - 6 months
--Foradil Aerolizer four months at room temperature

21

INTRANASAL INHALERS
**all products listed are administered with nasal spray dosage forms**
INTRANASAL CORTICOSTEROIDS
The primary indication for intranasal corticosteroids is allergic rhinitis. Allergic rhinitis is an
inflammation of the mucous membranes of the nose. Symptoms are a runny nose (clinical
term-rhinorrhea), nasal itching and sneezing.
Some trade name intranasal products are also indicated for prevention of recurrence of nasal
polyps following surgical removal.
Examples of intranasal corticosteroids:
1.
beclomethasone (Beconase AQ, Qnasl)
2.

triamcinolone (Nasacort AQ)

3.

budesonide (Rhinocort Aqua)

4.

flunisolide

5.

fluticasone (Flonase, Veramyst)


--Flonase contains the propionate salt
--Veramyst contains the furoate salt
--these products may not be substituted

6.

mometasone (Nasonex)

4.

ciclesonide (Omnaris)

Adverse effects reported with intranasal corticosteroids include nasal burning, nosebleed (clinical
term-epistaxis), and headache. Counsel patients that one or two weeks may be required before
maximum therapeutic benefit is achieved.
INTRANASAL MAST CELL STABILIZER
Intranasal mast cell stabilizers are indicated for allergic rhinitis. Mast cell stabilizers
reduce inflammation by inhibiting the release of inflammatory mediators from mast cells.
Two to three weeks may be required before maximum therapeutic benefit is achieved.
Example of intranasal mast cell stabilizer:
(1)
cromolyn (Nasalcrom)

22

INTRANASAL PITUITARY HORMONE

The antidiuretic hormone produced by the pituitary gland is vasopressin. Desmopressin is


synthetic vasopressin.
Examples of intranasal pituitary hormone:
(1)
desmopressin (DDAVP)
DDAVP is indicated for diabetes insipidus. This is a condition in which a
large volume of urine is produced due to a lack of vasopressin. DDAVP is
also indicated for primary nocturnal enuresis (bedwetting). Each spray of
DDAVP contains 10 mcg of desmopressin.
(2)

desmopressin (Stimate)
Stimate has a higher desmopressin concentration than DDAVP and is
indicated for prevention or treatment of bleeding in patients with hemophilia.
Stimate is not indicated for enuresis. Stimate increases levels of Clotting
Factor VIII and should be administered 2 hours preoperatively. Each spray
of Stimate contains 150 mcg of desmopressin.

INTRANASAL ANTICHOLINERGIC
Intranasal anticholinergics are indicated for allergic rhinitis.
Example of intranasal anticholinergic:
(1)
ipratropium (Atrovent Nasal Spray)
--2 available strengths:
-0.03% - for patients 6 to 12 years of age
-0.06% - for patients over 12 years of age
Adverse effects reported with intranasal anticholinergics include epistaxis and nasal dryness.
INTRANASAL ANTIHISTAMINE
Intranasal antihistamines are indicated for allergic rhinitis.
Example of intranasal antihistamines:
(1)
azelastine (Astepro)
INTRANASAL COMBINATION PRODUCT
Example of intranasal combination product containing an antihistamine and corticosteroid:
(1)
azelastine, fluticasone (Dymista)
--indicated for allergic rhinitis
INTRANASAL MEDICATION FOR OSTEOPOROSIS
This medication inhibits bone resorption.
Example: calcitonin (Miacalcin, Fortical)
Miacalcin and Fortical must be stored under refrigeration in the pharmacy. Patients may
store these products at room temperature for 35 days
23

NONSTEROIDAL ANTIINFLAMMATORY DRUGS (NSAIDS)


--analgesic, antiinflammatory, antipyretic
ibuprofen (Motrin)
naproxen sodium (Anaprox DS)
diclofenac sodium (Voltaren)
celecoxib (Celebrex)
nabumetone
etodolac
ketorolac
aspirin

naproxen (Naprosyn)
piroxicam (Feldene)
diclofenac potassium
meloxicam (Mobic)
indomethacin
oxaprozin
ketoprofen

--patient counseling - take with food


--NSAIDS cause GI irritation 2 ways:
1.
directly - food minimizes
2.
indirectly
phospholipase

cell membranes

arachidonic acid

cyclooxygenase -1
cytoprotective prostaglandins

cyclooxygenase-2

prostaglandins that cause inflammation

cytoprotective prostaglandins
1.
stimulate bicarbonate production
2.
stimulate mucous production
bicarbonate and mucous protect gastric cells from gastric acid
Ideally--NSAIDS should inhibit COX-2 and not COX-1. Most NSAIDS inhibit both
--indirect GI irritation of NSAIDS is cause by inhibiting COX - 1
--meloxicam, nabumetone, etodolac - more COX -2 selective
--celecoxib is a specific COX-2 inhibitor
Black Box Warnings:
--increase risk of cardiovascular events
--increase risk of GI bleeding
--do not use in patients allergic to aspirin

24

ketorolac
--same BBWs as other NSAIDS
--higher incidence of GI bleeding/ulceration
--only indicated for acute pain
--duration of therapy should not exceed 5 days
--four times daily
--two dosage forms:
--tablet
--maximum quantity - 20 tablets
--nasal spray (Sprix)
--package contains 5 single day bottles (8 sprays/bottle)
--after using the first spray discard bottle after 24 hours
diclofenac sodium
--enteric-coated tablet three times daily
--extended-release tablet - once daily
--ophthalmic four times daily
topical products
--topical solution (Pennsaid)
--indicated for arthritis of knee
--twice daily
--dimethyl sulfoxide (DMSO)
--topical gel (Voltaren Gel - 1%)
--indicated for arthritis joint pain
--four times daily
--dosing card measures either 2 or 4 grams
--4 grams/dose to lower extremities maximum daily dose 16 grams
--2 grams/dose to upper extremities maximum daily dose 8 grams
--Alcohol USP
--topical gel (Solaraze Gel - 3%)
--indicated for actinic keratosis (AK)
--actinic pertains to light rays
--keratosis growth on the skin
--twice daily
--another medication for AK (not an NSAID):
--imiquimod (Zyclara cream, Aldara cream) - category (immune response modifier)
--twice weekly

25

diclofenac potassium
--sugar-coated tablet
--indicated for pain
--three times daily
--powder for oral solution (Cambia)
--indicated for treatment of migraine headache
--50 mg packet - mix in 60 mL of water and drink immediately
--capsule (Zipsor)
--indicated for pain
--four times daily
diclofenac epolamine (Flector Patch)
--transdermal
--twice daily
--indicated for pain due to strains, sprains, bruises
Vimovo naproxen, esomeprazole
--naproxen - NSAID
--esomeprazole (Nexium - proton pump inhibitor PPI)
--indicated in patients taking NSAIDs long-term
--reduces the risk of NSAID induced ulcer formation
--twice daily
--take on empty stomach
Duexis - ibuprofen, famotidine
--ibuprofen - NSAID
--famotidine (Pepcid - H-2 Receptor Antagonist)
--indicated in patients taking NSAIDS long-term
--reduces the risk of NSAID induced ulcer formation
--three times daily
Durlaza - aspirin
--ER capsule
--platelet aggregation
Ophthalmic NSAIDS
--as a class ophthalmic NSAIDS are indicated for:
--allergic conjunctivitis
--inflammation following ocular surgery
--inhibition of intraoperative miosis
--miosis - pupil constriction
flurbiprofen (Ocufen)
diclofenac sodium
bromfenac
nepafenac (Nevanac, Ilevro)
ketorolac (Acular, Acuvail)
26

Cytotec - misoprostol
Arthrotec - misoprostol, diclofenac sodium
--indicated in patients taking NSAIDs long-term
--misoprostol is a prostaglandin
--reduces the risk of NSAID induced ulcer formation
--prevents indirect GI irritation
BBW for Cytotec and Arthrotec:
--do not use in pregnancy
--misoprostol is an abortifacient
--used with Mifeprex to induce abortions.
--Mifeprex - mifepristone
--indicated for termination of pregnancy
--Mifeprex has two therapeutic categories:
--abortifacient, antiprogestin
GOUT
--gout painful inflammation of a joint caused by uric acid crystals
-- hyperuricemia, podagra
causes

--poor uric acid excretion, diet (purines), diuretics

treatment
--NSAIDS, oral corticosteroids
--colchicine (Colcrys)
--therapeutic category - antiinflammatory
--dose/dosing interval for acute attack
1.2 mg (2 tablets) stat, then 1 tablet in 1 hour
--pegloticase (Krystexxa)
--indicated for treatment resistant gout
--pegloticase - uric acid specific enzyme - metabolizes uric acid to allantoin
--parenteral (IV)
--every 2 weeks
--BBW - severe allergic reactions
prevention
--diet modifications
--medications:
--febuxostat (Uloric), allopurinol (Zyloprim)
--once daily
--therapeutic category xanthine oxidase inhibitors
--colchicine (Colcrys)
--0.6 mg twice daily
27

ANTIRETROVIRAL AGENTS
--indicated for human immunodeficiency virus (HIV)
--T cells are part of immune system
--as HIV progresses - fewer T cells, increased viral load
--HIV enters T cells through two receptors:
--CCR5 receptor
--CXCR4 receptor
Five classes of antiretrovirals:
Reverse Transcriptase Inhibitors
Protease Inhibitors
Integrase Inhibitors
CCR5 Antagonists
Fusion Inhibitors
--HAART (highly active antiretroviral therapy)
--at least two antiretroviral classes
Reverse Transcriptase Inhibitors
1. Nucleoside Reverse Transcriptase Inhibitors
Retrovir - zidovudine (AZT)
stavudine (d4T)
Epivir - lamivudine (3TC)
Tyzeka - telbivudine
Videx EC - didanosine (ddI)
Ziagen abacavir
Emtriva - emtricitabine
2. Non-Nucleoside Reverse Transcriptase Inhibitors
Viramune nevirapine Rescriptor delavirdine
Sustiva efavirenz
Intelence etravirine
Edurant - rilpivirine
3. Nucleotide Reverse Transcriptase Inhibitors
Viread - tenofovir
4. Reverse Transcriptase Inhibitors Combination Products
Truvada - emtricitabine, tenofovir
Atripla - efavirenz, emtricitabine, tenofovir
Combivir - zidovudine, lamivudine
Epzicom - abacavir, lamivudine
Trizivir - abacavir, lamivudine, zidovudine
Complera emtricitabine, rilpivirine, tenofovir
28

Protease Inhibitors
Viracept nelfinavir
Invirase - saquinavir
Crixivan - indinavir
Aptivus tipranavir

Lexiva - fosamprenavir
Norvir - ritonavir
Reyataz - atazanavir
Prezista-darunavir

Protease Inhibitor Combination Products


Kaletra - lopinavir, ritonavir
Evotaz - atazanavir, cobicistat
Prezcobix - darunavir, cobicistat
Tybost - cobicistat
--pharmacokinetic enhancer
--enhances effects of atazanavir and darunavir
Integrase Inhibitors
Isentress - raltegravir
Tivicay - dolutegravir
Vitekta - elvitegravir
Integrase Inhibitor Combination Products
Triumeq - abacavir, dolutegravir, lamuvidine
Stribild, Genvoya - elvitegravir, cobicistat, emtricitabine, tenofovir
CCR5 Antagonists
Selzentry maraviroc
Fusion Inhibitors
--Fuzeonenfuvirtide
--subcutaneous injection
Antiretroviral patient counseling
1.
take exactly as prescribed
2.
Invirase and Aptivus
--take with food
--take with ritonavir
3.
Prezista and Reyataz
--take with food
--take with ritonavir or cobicistat
4.
Kaletra (lopinavir, ritonavir)
--take with food
Truvada (emtricitabine, tenofovir) indicated for pre-exposure prophylaxis
--reduces risk of HIV in high risk adults

29

ANTIVIRAL AGENTS

--acyclovir - Zovirax
--famciclovir - Famvir
--valacyclovir - Valtrex
--valacyclovir is converted to acyclovir

--acyclovir, famciclovir, valacyclovir indicated for:


--herpes zoster (shingles)
--varicella - zoster virus
--herpes genitalis (genital herpes)
--herpes simplex virus -2 (HSV-2)
--herpes labialis (cold sores - fever blisters)
--herpes simplex virus -1 (HSV-1)
--acyclovir, valacyclovir are indicated for chickenpox
--varicella-zoster virus
--dosing intervals and durations of therapy for herpes labialis:
--oral and topical (5%) Zovirax 5X daily for 5 days
--Famvir - single 1,500 mg dose
--Valtrex - 2 grams twice daily for 1 day
--antiviral creams:
--Denavir penciclovir--Rx
--Abreva docosanol --OTC
--buccal tablet
--Sitavig - acyclovir - Rx
--oseltamivir (Tamiflu) zanamivir (Relenza) amantadine rimantadine (Flumadine)
--all indicated for treatment and prevention of influenza
--Tamiflu and Relenza - neuraminidase inhibitors
--Tamiflu:
--2 dosage forms
--capsule (30 mg, 45 mg, 75 mg), powder for oral suspension (6 mg/mL)
--dose/dosing interval:
--patients 13 and over (75 mg), patients under 13 - dose based on weight
--treatment of influenza - twice daily for 5 days
--prevention of influenza - once daily for 10 days
30

--Relenza
--dry powder inhaler (Diskhaler)
--dose/dosing interval
--treatment of influenza (7 years and older)
--10 mg twice daily for 5 days
--prevention of influenza in household setting (5 years and older)
--10 mg once daily for 10 days
--prevention of influenza in community outbreak (5 years and older)
--10 mg once daily for 28 days
--amantadine, rimantadine (Flumadine)
ANTIPARKINSONS AGENTS
--neurological disorder caused by low dopamine levels
--amantadine
--levodopa
--carbidopa, levodopa (Sinemet)
--levodopa, carbidopa, entacapone (Stalevo)
--ropinirole (Requip)
--pramipexole (Mirapex)
--selegiline
--capsule (Eldepryl) ODT (Zelapar)
--amantadine
--Antiviral Agent, Antiparkinsons Agent
--levodopa
--converted to dopamine in the brain
--administered in combination with carbidopa (Sinemet)
--carbidopa prevents peripheral breakdown of levodopa
--Stalevo (levodopa, carbidopa, entacapone)
--entacapone prevents peripheral breakdown of levodopa
--ropinirole (Requip)
--pramipexole (Mirapex)
--dopamine receptor agonists
--also indicated for Restless Legs Syndrome (RLS)
--selegiline (Eldepryl, Zelapar)
--raise dopamine levels
--patient counseling:
--levodopa should not be administered within 2 hours of iron products
--Mirapex, Requip take with food

31

ALZHEIMER'S DISEASE

Cholinesterase Inhibitors
donepezil (Aricept)
--tablet (5 mg, 10 mg, 23 mg)
galantamine (Razadyne, Razadyne ER)
--tablet, ER capsule
rivastigmine (Exelon)
--capsule, transdermal

NMDA Receptor Antagonists


memantine (Namenda, Namenda XR)
--glutamate
--tablet (5 mg, 10 mg), ER capsule (7 mg, 14 mg, 21 mg, 28 mg)
--tablet - twice daily
--extended-release capsule - once daily
--initial dose 7 mg - increase by 7 mg weekly prn
--maximum recommended daily dose - 28 mg
Namzaric (donepezil, memantine)
--once daily
IRRITABLE BOWEL SYNDROME
abdominal pain with altered bowel movements
--constipation predominant, diarrhea predominant
treatment of diarrhea predominant IBS
anticholingerics
hyoscyamine (Levsin, Anaspaz)
dicyclomine (Bentyl)
glycopyrrolate (Robinul)
clidinium (Librax - chlordiazepoxide, clidinium)
alosetron (Lotronex)
--selective serotonin receptor antagonist
--restricted dispensing program
rifaximin (Xifaxan)
--antibiotic
--also indicated for Traveler's Diarrhea caused by E.Coli
eluxadoline (Viberzi)
--opioid receptor agonist

32

treatment of constipation predominant IBS


chloride channel activator
Amitiza lubiprostone (8 mcg, 24 mcg)
--constipation predominant IBS (8 mcg BID)
--chronic constipation (24 mcg BID)
--opioid induced constipation (24 mcg BID)
guanylate cyclase-C agonist
--Linzess linaclotide (145 mcg, 290 mcg)
--constipation predominant IBS (290 mcg daily)
--chronic constipation (145 mcg daily)
patient counseling:
anticholinergics - xerostomia, constipation, sedation, mydriasis, oligohidrosis
Amitiza - take with food
Linzess - original container, take on empty stomach
Viberzi - take with food
OVERACTIVE BLADDER
--incontinence - involuntary discharge of urine
--urgency - a sudden urge to urinate
--frequency - urination at short intervals
--micturition
--tolterodine
--anticholinergic
--IR tablet (Detrol), ER capsule (Detrol LA)
--oxybutynin
--anticholinergic
--IR tablet, ER tablet (Ditropan XL)
--topical gel (10%) Gelnique
--once daily
--alcohol USP
--transdermal (Oxytrol)
--twice weekly
--trospium
--anticholinergic
--IR tablet, ER capsule
--patient counseling - take on empty stomach
--darifenacin (Enablex)
solifenacin (Vesicare)
--all anticholingerics

fesoterodine (Toviaz)

--patient counseling for anticholinergics:


--xerostomia, constipation, sedation, mydriasis, oligohidrosis
--mirabegron (Myrbetriq) - beta 3 agonist
33

ANTIFUNGALS

topical fungal infections


--tinea corporis (ringworm) - zoonotic
--tinea cruris (jock itch)
topical antifungals:
Tinactin (tolnaftate)
ciclopirox
Lamisil AT (terbinafine)
Lotrimin Ultra, Mentax (butenafine)

tinea pedis (athletes foot)


tinea unguium (onychomycosis)
Lotrimin AF (clotrimazole)
ketoconazole
econazole
Ertaczo (sertaconazole)

Penlac Nail Lacquer (ciclopirox)


--indicated for onychomycosis - once daily
Jublia (efinaconazole)
--indicated for onychomycosis - once daily
Kerydin - tavaborole
--indicated for onychomycosis - once daily
systemic fungal infections
--two classes of oral antifungals:
--triazoles:
--fluconazole (Diflucan)
--voriconazole (Vfend)

itraconazole (Sporanox)
posaconazole (Noxafil)

--imidazoles:
--ketoconazole, clotrimazole, miconazole
--two other oral antifungals :
--griseofulvin (Gris-PEG)
--terbinafine (Lamisil )
--SALAD with Lamictal - lamotrigine (anticonvulsant)
--patient counseling for oral antifungals
--finish medication
--take griseofulvin with food
--take ketoconazole 2 hours before antacids

34

TRANSDERMAL DRUG DELIVERY SYSTEMS


advantages
--avoid first pass effect by the liver
--compliance

two types of transdermal systems


--adhesive matrix
--reservoir

transdermal "strengths" expressed as release rates:


ex: medication name/strength/time
--fentanyl 25 mcg/hour
nitroglycerin transdermal systems
--trade names:
--Minitran, Nitro-Dur
--adhesive matrix systems
--available in several release rates (ex: Minitran 0.1mg/hour)
--indicated for prevention of angina pectoris
--once daily
--tolerance
--headache
--ranolazine (Ranexa)
--tablet
--indicated for prevention of angina pectoris
--twice daily

35

ESTRADIOL PRODUCTS
Estradiol is an estrogen hormone indicated for hormone replacement therapy (HRT) in
postmenopausal women. Loss of ovarian estrogen secretion after menopause may result in
instability of thermoregulation causing hot flashes associated with sleep disturbance and
excessive sweating. Estradiol is indicated for vasomotor symptoms (hot flashes) and vaginal
atrophy associated with menopause. Estradiol is also indicated for prevention of osteoporosis.
Specific indications vary between products.
estradiol transdermal systems
Climara
0.025 mg/24 hours
0.0375 mg/24 hours
0.05 mg/24 hours
0.06 mg/24 hours
0.075 mg/24 hours
0.1 mg/24 hours
Vivelle DOT
0.025 mg/24 hours
0.05 mg/24 hours
0.1 mg/24 hours
Alora
0.025 mg/24 hours
0.075 mg/24 hours
Minivelle
0.0375 mg/24 hours
0.05 mg/24 hours
0.075 mg/24 hours
0.1 mg/24 hours

0.0375 mg/24 hours


0.075 mg/24 hours
0.05 mg/24 hours
0.1 mg/24 hours
Menostar
0.014 mg/24 hours

estradiol transdermal spray


Evamist
estradiol topical gel
Divigel (0.1% strength)
3 packet sizes
0.25 grams (0.25 mg estradiol)
0.5 grams (0.5 mg estradiol)
1 gram (1 mg estradiol)

estradiol vaginal ring


Femring
0.05 mg/24 hours
0.1 mg/24 hours

estradiol vaginal tablet


Vagifem
10 mcg

estradiol vaginal cream


Estrace
0.1 mg/gram

estradiol combination products


ClimaraPro (estradiol, levonorgestrel)

CombiPatch (estradiol, norethindrone)


36

ESTRADIOL PRODUCTS
estradiol Black Box Warnings:
--increased risk of cardiovascular disease and dementia in postmenopausal women
--increased risk of endometrial cancer in younger women
--do not use in patients with a history of breast cancer
estradiol transdermal systems
--all adhesive matrix
--all indicated for vasomotor symptoms, vaginal atrophy, osteoporosis
--except Menostar
Climara
--6 release rates
--0.025 mg/24 hours
0.0375 mg/24 hours
--0.05 mg/24 hours
0.06 mg/24 hours
--0.075 mg/24 hours
0.1 mg/ 24 hours
--dosing interval - once weekly
Vivelle-Dot
--5 release rates
--0.025 mg/24 hours
0.0375 mg/24 hours
--0.05 mg/24 hours
0.075 mg/24 hours
--0.1 mg/24 hours
--dosing interval - twice weekly
Alora
--4 release rates
--0.025 mg/24 hours
0.05 mg/24 hours
--0.075 mg/24 hours
0.1 mg/24 hours
--dosing interval - twice weekly
Minivelle
--4 release rates
--0.0375 mg/24 hours 0.05 mg/24 hours
--0.075 mg/24 hours
0.1 mg/24 hours
--dosing interval - twice weekly
Menostar
--0.014 mg/24 hours
--only indicated for osteoporosis
--dosing interval - once weekly

37

estradiol transdermal spray (Evamist)


--indicated for vasomotor symptoms, vaginal atrophy, osteoporosis
--alcohol USP, octisalate
--spray on inside of forearm
--once daily
estradiol topical gel (Divigel)
--indicated for vasomotor symptoms, vaginal atrophy, osteoporosis
--3 packet sizes:
--0.25 gram packet contains 0.25 mg estradiol
--0.5 gram packet contains 0.5 mg estradiol
--1 gram packet contains 1 mg estradiol
--alcohol USP
--apply contents of one packet to thigh
--once daily
estradiol vaginal ring (Femring)
--indicated for vasomotor symptoms, vaginal atrophy, osteoporosis
--two strengths:
--0.05 mg/24 hours
--0.1 mg/24 hours
--inserted vaginally
--every three months
estradiol vaginal tablet (Vagifem)
--indicated for vaginal atrophy
--10 mcg
--inserted vaginally with an applicator
--initial dosing interval once daily for two weeks
--maintenance dosing interval twice weekly
estradiol vaginal cream (Estrace)
--indicated for vaginal atrophy
--0.1 mg of estradiol/gram of cream
--applicator calibrated in 1 gram increments to a maximum of 4 grams
--dosing interval - variable
conjugated equine estrogens (Premarin Vaginal Cream)
--indicated for vaginal atrophy
--0.625 mg/gram of cream
--applicator calibrated in 0.5 g increments to a maximum of 2 grams
--twice weekly

38

estradiol combination products


Climara Pro - estradiol, levonorgestrel
--levonorgestrel is a progestin
--synthetic progesterone
--indicated for vasomotor symptoms, osteoporosis
--once weekly
CombiPatch - estradiol, norethindrone
--norethindrone is a progestin
--indicated for vasomotor symptoms, vaginal atrophy, osteoporosis
--store in refrigerator in pharmacy
--patients store at room temperature for up to three months
--twice weekly
--same ingredients in an oral tablet dosage form - Activella
--indicated for vasomotor symptoms, vaginal atrophy, osteoporosis
--0.5 mg estradiol, 0.1 mg norethindrone
--1 mg estradiol, 0.5 mg norethindrone
--once daily
Xulane - norelgestromin, ethinyl estradiol
--norelgestromin is a progestin
--indicated for contraception
--once weekly
--three weeks patch on - one week patch off

39

TESTOSTERONE PRODUCTS
men normally produce 5 mg of testosterone daily
synthetic derivatives of testosterone are anabolic steroids
--Anabolic Steroids Control Act
--testosterone products DEA CIII substances
testosterone products are indicated for male hypogonadism
--insufficient secretion of testosterone
--decreased libido, loss of energy
testosterone is available in four dosage forms:
--transdermal, topical gel, topical solution, injection (IM)
testosterone transdermal system (Androderm)
--reservoir system
--alcohol USP
--available in 2 release rates:
--2 mg/24 hours, 4 mg/24 hours
--once daily
testosterone gel
--3 trade names available (Androgel, Testim, Fortesta)
--all contain alcohol USP
Androgel
--available in two different delivery systems:
single dose packets of gel
1% gel
2 package sizes:
--2.5 g contains 25 mg testosterone
--5 g contains 50 mg of testosterone
--absorb 10% of the dose (2.5 mg or 5 mg)
1.62% gel
2 package sizes:
--1.25 g contains 20 mg testosterone
--2.5 g contains 40 mg testosterone
--absorb 10% of dose (2 mg or 4 mg)
--metered dose pump
--1.62% (20 mg testosterone/pump)
--dose is 2 pumps (40 mg testosterone)
--absorb 10% (4 mg)
--once daily

40

Testim

--single dose packets of gel


--each packet 50 mg of testosterone
--absorb 10% (5 mg)
--once daily

Fortesta
--metered dose pump
--10 mg of testosterone/pump
--dose is 4 pumps (40 mg of testosterone)
--absorb 10% (4 mg)
--apply 2 pumps to each thigh
--once daily
testosterone topical solution (Axiron)
--metered dose pump
--alcohol USP
--30 mg of testosterone/pump
--dose is 2 pumps (60 mg)
--absorb 10% (6 mg)
--apply 1 pump under each arm
--once daily
testosterone injection (parenteral)
--intramuscular injection (IM)
--100 mg/mL, 200 mg/mL
--dosing interval - every 2 or 4 weeks
topical testosterone BBW:
--secondary exposure may cause virilization in children and women
drug interactions - anticoagulants, insulin

41

CLONIDINE TRANSDERMAL
--trade name - Catapres TTS
--therapeutic category - antihypertensive
--TTS = transdermal therapeutic system
--reservoir system
--alcohol USP
--3 release rates:
--0.1 mg/24 hours, 0.2 mg/24 hours, 0.3 mg/24 hours
--start with 0.1 mg system - increase by 0.1 mg at weekly intervals prn
--once weekly
--overlay covers
--clonidine ER tablets are indicated for ADHD
--Kapvay
FENTANYL TRANSDERMAL

--trade name - Duragesic


--therapeutic category - opioid analgesic
--all fentanyl products are CII
--indicated for chronic pain
--reservoir system (alcohol USP)

--dosing interval - every 3 days (72 hours)


--Duragesic has 5 release rates:
--12.5 mcg/hour, 25 mcg/hour, 50 mcg/hour, 75 mcg/hour, 100 mcg/hour
--three other generic release rates:
--37.5 mcg/hour, 62.5 mcg/hour, 87.5 mcg/hour
--Duragesic is not indicated for acute or breakthrough pain
--fentanyl is available in 5 other dosage forms to treat breakthrough pain
--use in patients on chronic opioid therapy
--4 transmucosal systems, one nasal spray
--all have onsets of action in ~15 minutes
fentanyl transmucosal systems
--fentanyl lozenge (Actiq)
--fentanyl buccal tablet (Fentora)
--fentanyl sublingual tablet (Abstral)
--fentanyl sublingual spray (Subsys)
fentanyl nasal spray (Lazanda)
42

SCOPOLAMINE, TRANSDERMAL
--trade name - Transderm-Scop
--apply to a hairless area behind the ear
--release rate - 5 mcg/hour
--two indications:
--prevention of nausea and vomiting associated with motion sickness
--apply one system at least 4 hours before antiemetic effect is required
--may leave in place for up to 3 days
--if required after 3 days - remove and place a new system behind other ear
--prevention of nausea/vomiting after anesthesia during surgery
PRODUCTS FOR SMOKING CESSATION
2 types oral medications, nicotine replacement products
Oral medications
--Zyban - bupropion (aminoketone antidepressant)
--ER tablet (150 mg)
--150 mg daily for 3 days, then twice daily for 12 weeks
--Chantix--varenicline
--therapeutic category - nicotine receptor agonist
--produces nicotine-like effects
--inhibits nicotine binding at nicotine receptor
--tablet (0.5 mg, 1 mg)
--0.5 mg daily for 3 days
--0.5 mg twice daily for 4 days
--1 mg twice daily for 12 weeks
--after 12 weeks, reevaluate
--adverse effects:
--nausea, unusual dreams, violent behavior
--BBW:
--may cause neuropsychiatric events
Nicotine replacement products
--dosage forms - transdermal, gum, inhaler, lozenge

Nicotine transdermal system


--Nicoderm CQ
--adhesive matrix
--21mg/24hours, 14mg/24 hours, 7mg/24 hours
--dosing interval - once daily
--dosing schedules:
--if patient smokes over10 cigarettes/day:
--21 mg system for 6 weeks, 14 mg system for 2 weeks, 7 mg system for 2 weeks
--if patient smokes 10 cigarettes or less/day:
--14 mg for 6 weeks, 7 mg for 2 weeks
43

Nicotine gum
--Nicorette (2 mg), Nicorette DS (4 mg)
--smoke more than 25 cigarettes per day (4 mg)
--less than 25 per day (2 mg)
--alkaline saliva
--do not chew continuously
Nicotine lozenge
--2 mg, 4 mg strengths
--dosed based on time to first cigarette
--if smoke within 30 minutes of awakening - 4 mg
--if smoke after 30 minutes - 2 mg
--dosing interval for both strengths
--one every 1-2 hours for 6 weeks
--one every 2-4 hours for 3 weeks
--one every 4-8 hours for 3 weeks
--alkaline saliva
Nicotine inhaler (Nicotrol Inhaler)
--Rx only
--each cartridge contains 4 mg nicotine
--duration of treatment - 12 weeks
--after 12 weeks - reevaluate patient

LIDOCAINE TRANSDERMAL

--therapeutic category - local anesthetic


--Lidoderm
--5% lidocaine
--indicated for pain associated with post-herpetic neuralgia (PHN)
--clinical term for shingles - herpes zoster
--diagnosis of PHN is made if pain persists for 3 months after blisters have healed
--Lidoderm is not indicated for use during shingles outbreak
--once daily
--apply up to 3 patches to affected area
--patch on period - 12 hours
--patch off period - 12 hours
OXYBUTYNIN TRANSDERMAL
--therapeutic category - anticholinergic
-- Oxytrol
--OTC
--adhesive matrix
--indicated for overactive bladder
--twice weekly
44

METHYLPHENIDATE TRANSDERMAL
--therapeutic category - CNS Stimulant
--Daytrana - CII
--10 mg/9 hours, 15 mg/9 hours, 20 mg/9 hours, 30 mg/9 hours
--adhesive matrix
--indicated for ADHD and narcolepsy
--once daily
--apply 2 hours before effect needed
--remove 9 hours after application
GRANISETRON TRANSDERMAL
--therapeutic category - antiemetic
--Sancuso
--adhesive matrix
--indicated for nausea/vomiting in patients receiving chemotherapy for up to 5
consecutive days
--chemoreceptor trigger zone (CTZ)
--once weekly
--apply patch 24 hours before the first chemo treatment
--leave patch on 24 hours after the last chemo treatment
--patch can be worn up to 7 days
--phototoxic reactions
RIVASTIGMINE TRANSDERMAL
--therapeutic category cholinesterase inhibitor
--Exelon Patch
--4.6 mg/24 hours, 9.5 mg/24 hours, 13.3 mg/24 hours
--adhesive matrix
--indicated for Alzheimers Disease
--increases acetylcholine levels
--once daily
--adverse effects - nausea/vomiting
--start all patients on the 4.6 mg/24 hours release rate for 4 weeks
--increase to 9.5 mg/24 hours
--after 4 weeks increase to 13.3 mg/24 hours prn
--4.6 mg/24 hours is the initial dose
--9.5 mg/24 hours and 13.3 mg/24 hours are maintenance doses
--oral cholinesterase inhibitors
--donepezil (Aricept)
--galantamine (Razadyne)

45

BUPRENORPHINE TRANSDERMAL
--therapeutic category opioid analgesic
--Butrans - CIII
--5 mcg/hour, 10 mcg/hour, 20 mcg/hour
--adhesive matrix
--indicated for patients requiring around-the-clock pain control
--once a week
--dont use same application site for 21 days
DICLOFENAC EPOLAMINE TRANSDERMAL
--therapeutic category NSAID
--Flector
--adhesive matrix
--indicated for pain due to muscle strains, sprains, bruises
--decreases prostaglandin formation
--twice daily

46

ANTIHYPERLIPIDEMICS

hyperlipidemia
lipoproteins
--high density lipoproteins (HDL)
--low density lipoproteins (LDL)
hypertriglyceridemia
goal of therapy:
--lower LDL, lower triglycerides, raise HDL
--optimal LDL level - less than 100 mg/dL
--high risk patients LDL below 70 mg/dL
--optimal HDL level - above 40 mg/dL
--optimal triglyceride level - less than 150 mg/dL
fluvastatin (Lescol)
pravastatin (Pravachol)
atorvastatin (Lipitor)
rosuvastatin (Crestor)
lovastatin (Mevacor, Altoprev)
fenofibrate (Tricor, Triglide, Lofibra, Antara)
cholestyramine (Questran, Prevalite)
colesevelam (Welchol)
atorvastatin, amlodipine (Caduet)
ezetimibe, simvastatin (Vytorin)
omega-3 fatty acids (Lovaza)

simvastatin (Zocor)
pitavastatin (Livalo)
gemfibrozil (Lopid)
fenofibric acid (Trilipix)
colestipol (Colestid)
lovastatin, niacin (Advicor)
ezetimibe (Zetia)
niacin, simvastatin (Simcor)
icosapent (Vascepa)

Lescol, Pravachol, Zocor, Lipitor, Crestor, Livalo, Mevacor, Altoprev


--antihyperlipidemic class - HMG-CoA Reductase Inhibitors (statins)
--patient counseling:
--rhabdomyolysis
--to not take during pregnancy
--IR lovastatin (Mevacor) with food
--ER lovastatin (Altoprev) on empty stomach
Lopid, Tricor, Triglide, Lofibra, Trilipix, Antara
--antihyperlipidemic class - Fibric Acid Derivatives
--caution with HMG-CoA Reductase Inhibitors
--Trilipix is the only fibric acid derivative approved for use with a "statin"
--fenofibric acid active metabolite of fenofibrate
--patient counseling: take Lopid on empty stomach
Questran, Prevalite, Colestid, Welchol
--antihyperlipidemic class - Bile Acid Sequestrants.
--patient counseling:
--may cause constipation, take with plenty of water, bind to other medications
--Welchol also indicated for Type 2 diabetes
--tablet (625 mg) 3 tablets twice daily or 6 tablets as a single dose
--powder for oral suspension
--3.75 grams (once daily)
47

Zetia (ezetimibe) --antihyperlipidemic class - Cholesterol Absorption Inhibitors


Advicor (IR lovastatin, niacin)
--niacin (Niaspan)
--patient counseling:
--take with food, 325 mg aspirin or 200 mg ibuprofen
Caduet (atorvastatin, amlodipine)
Vytorin (ezetimibe, simvastatin)
Simcor (niacin, simvastatin)
--patient counseling with Simcor:
--take with food, 325 mg aspirin or 200 mg ibuprofen
Lovaza (omega-3 fatty acids)
--three omega-3 fatty acids
--Lovaza contains EPA, DHA
--indicated for severe hypertriglyceridemia
--1 gram capsule
--four grams per day (two capsules twice daily or four as a single dose)
Vascepa (icosapent)
--contains EPA
--indicated for severe hypertriglyceridemia
--1 gram capsule (same dosing options as Lovaza)
ANTIARRHYTHMICS
amiodarone (Cordarone, Pacerone) dronedarone (Multaq)
disopyramide (Norpace)
flecainide
mexiletine
propafenone (Rythmol)
dofetilide (Tikosyn)
patient counseling:
--BBW - proarrhythmic effects
three antiarrhythmics have other Black Box Warnings
amiodarone
--proarrhythmic effects
--use in patients with life-threatening arrhythmias
--pulmonary toxicity (alveolitis)
dronedarone
--proarrhythmic effects
--use cautiously in patients with severe heart failure
dofetilide
--proarrhythmic effects
--monitor continuous ECG for three days
--use in patients with life-threatening arrhythmias
48

DIGOXIN
--indicated for heart failure - positive inotropic action
--dosage forms
--tablet (Lanoxin)
--0.0625 mg (peach) 0.125 mg (yellow)
--0.1875 mg (blue)
0.25 mg (white)
--oral solution - 0.05 mg/mL
--parenteral (Lanoxin) - 0.25 mg/mL
digoxin therapeutic serum level:
--heart failure 0.5 1 ng/mL
arrhythmias 0.8 - 2 ng/mL
patient counseling:
--may cause nausea, vomiting, or vision problems
Entresto (sacubitril, valsartan)
--indicated for heart failure
--natriuretic peptides (cardioprotective)
--valsartan - angiotensin II receptor antagonist (ARB)
--sacubitril - neprilysin inhibitor
--inhibit neprilysin - increase levels of natriuretic peptides
BENZODIAZEPINES
anxiolytic benzodiazepines
--anxiolytic - medication that reduces anxiety
--alprazolam
--IR tablet (Xanax)
--ER tablet (Xanax XR)
--clorazepate
diazepam (Valium)
--lorazepam (Ativan) oxazepam
chlordiazepoxide
anticonvulsant/antipanic benzodiazepines
--clonazepam (Klonopin)
--indicated for absence seizures, Lennox-Gastaut, panic disorder
--IR tablet Klonopin
--orally-disintegrating tablet
--SALAD with clonidine (Catapres)
hypnotic benzodiazepines
--flurazepam temazepam (Restoril) triazolam (Halcion) estazolam
Patient counseling:
--somnolence
--avoid alcohol
--don't discontinue abruptly
--may affect memory
--anterograde amnesia, retrograde amnesia
49

NON-BENZODIAZEPINE HYPNOTICS
Rozerem (ramelteon)
--non-benzodiazepine hypnotic class - melatonin receptor agonist
Lunesta (eszopiclone)
--non-benzodiazepine hypnotic class - cyclopyrrolone
--bitter aftertaste
zolpidem
--non-benzodiazepine hypnotic class - imidazopyridine
--IR tablet Ambien (5 mg, 10 mg)
--ER tablet Ambien CR (6.25 mg, 12.5mg)
--sublingual tablet
--Edluar (5 mg, 10 mg)
--Intermezzo
--men 3.5 mg
--women 1.75 mg
--oral solution Zolpimist (5 mg/spray)
Sonata (zaleplon)
--non-benzodiazepine hypnotic class - pyrazolopyrimidine
Belsomra (suvorexant)
--non-benzodiazepine hypnotic class - orexin receptor antagonist
Patient Counseling:
--sleepwalking (somnambulism)
--avoid alcohol
ANTIDEPRESSANTS
--all antidepressants have a BBW:
--increase risk of suicidal thinking in patients under 24 with depression or other
psychiatric disorders
--dysthymia chronic low-grade depression
1.

triazolopyridines
trazodone
--indicated for depression
--tablet, ER tablet (Oleptro)
2.

tetracyclics
mirtazapine
--indicated for depression
--tablet (Remeron), orally disintegrating tablet (Remeron SolTab)

50

3.

aminoketones
bupropion
--indicated for depression, seasonal affective disorder (SAD)
--smoking cessation
--trades indicated for depression and SAD:
--Wellbutrin - three times daily
--Wellbutrin SR - twice daily
--Wellbutrin XL - once daily
--trade indicated for smoking cessation - Zyban

4.

phenylpiperazines
nefazodone
--indicated for depression

5.

selective norepinephrine and serotonin reuptake inhibitors (SNRIs)


venlafaxine (Effexor)
--indicated for depression, anxiety, panic disorder
desvenlafaxine (Pristiq)
--indicated for depression
duloxetine (Cymbalta)
--indicated for depression, anxiety, fibromyalgia
--pain associated with diabetic peripheral neuropathy (DPN)
--chronic musculoskeletal pain
--pain associated with osteoarthritis
milnacipran (Savella) - indicated for fibromyalgia
levomilnacipran (Fetzima) - indicated for depression

6.

selective serotonin reuptake inhibitors (SSRIs)


fluoxetine (Prozac)
paroxetine hydrochloride (Paxil)
paroxetine mesylate (Pexeva)
paroxetine (Brisdelle)
--only indicated for vasomotor symptoms
sertraline (Zoloft)
fluvoxamine
--only indicated for obsessive compulsive disorder (OCD)
citalopram (Celexa)
escitalopram (Lexapro)
vortioxetine (Brintellix)
vilazodone (Viibryd)

51

--SSRI's have a variety of indications:


--specific indications vary from drug to drug
--depression, OCD, panic disorder, anxiety
--post-traumatic stress disorder (PTSD)
--premenstrual dysphoric disorder (PMDD)
--medications indicated for PMDD
--fluoxetine, Zoloft, Paxil, Yaz
-Yaz (drospirenone, ethinyl estradiol)
7.

tricyclics
amitriptyline
clomipramine [Anafranil (only indicated for OCD)]
doxepin [Silenor (only indicated for insomnia)]
desipramine (Norpramin)
imipramine (Tofranil)
nortriptyline (Pamelor)

Patient counseling for antidepressants:


--somnolence, avoid alcohol
--use good dental care (dry mouth - xerostomia)
--two medications indicated for xerostomia:
--Evoxac (cevimeline) Salagen (pilocarpine)
--therapeutic category - cholinergic agents
--also used in the treatment of Sjogrens syndrome
MONOAMINE OXIDASE INHIBITORS (MAOIS)
therapeutic category antidepressant
--phenelzine (Nardil)
--isocarboxazid (Marplan)
--tranylcypromine (Parnate)
--selegiline (Emsam)
BBW:
--increased risk of suicidal thinking in patients under 24 with depression
Patient counseling:
--avoid foods and drinks containing large amounts of tyramine
--hypertensive crisis
--tyramine is a sympathomimetic
--do not take nasal decongestants
--pseudoephedrine, phenylephrine
--do not take other antidepressants
--patient switching to an MAOI from another antidepressant
--wait two weeks before starting the MAOI
--wait five weeks if switching from fluoxetine
--patient switching to another antidepressant from an MAOI
--wait two weeks before starting the other antidepressant
52

selegiline (Emsam)
--transdermal delivery system
--once daily
--more centrally selective - less risk of hypertensive crisis
--release rates: 6 mg/24h, 9 mg/24 hours, 12 mg/24 hours
--patients using 9 mg/24h and 12 mg/24h should avoid tyramine
--OTC decongestants should be avoided with all strengths
--selegiline available in two other dosage forms:
--capsule (Eldepryl)
--orally disintegrating tablet (Zelapar)
--both indicated for Parkinson's Disease
ANTIPSYCHOTICS
--two primary indications:
(1) schizophrenia
--disorder characterized by delusions, hallucinations, bizarre behavior, and
dereistic thinking (dereistic disconnected from reality)
(2) bipolar disorder
--BBW:
--do not use in the elderly with dementia
--two main types:
Atypical - novel

Typical - conventional

Atypical Antipsychotics
aripiprazole
--schizophrenia, bipolar disorder, irritability associated with autism
--Tourette's Syndrome
--adjunctive therapy for depression
--tablet (Abilify)
--orally disintegrating tablet (Abilify Discmelt)
brexpiprazole (Rexulti)
--schizophrenia, bipolar disorder,
--adjunctive therapy for depression
quetiapine (Seroquel)
--schizophrenia, bipolar disorder
--adjunctive therapy for depression
asenapine (Saphris)
--schizophrenia, bipolar disorder
--sublingual tablet
53

olanzapine
--schizophrenia, bipolar disorder
--tablet (Zyprexa)
--orally disintegrating tablet (Zyprexa Zydis)
risperidone (Risperdal)
--schizophrenia, bipolar disorder, irritability associated with autism
--tablet (Risperdal)
--orally disintegrating tablet (Risperdal M-Tab)
paliperidone (Invega)
--schizophrenia
--active metabolite of risperidone
iloperidone (Fanapt)
lurasidone (Latuda)
--both indicated for schizophrenia
ziprasidone (Geodon)
--schizophrenia, bipolar disorder
clozapine (Clozaril)
--indicated for treatment resistant schizophrenia
--tablet (Clozaril)
--orally-disintegrating tablet (FazaClo)
--BBWs:
--agranulocytosis
--increased seizure risk
--severe orthostatic hypotension
--syncope
--midodrine - vasopressor, antihypotensive agent
Atypical antipsychotics associated with three problems:
--weight gain, increased risk of diabetes, increased risk of hyperlipidemia
Typical antipsychotics
phenothiazines
--chlorpromazine
--trifluoperazine
butyrophenones
--haloperidol
lithium

perphenazine
prochlorperazine

--therapeutic category antimanic agent

patient counseling for antipsychotics - somnolence, avoid alcohol


54

thioridazine
fluphenazine

OPIOID ANALGESICS
(1) meperidine (Demerol) - CII
(2) hydromorphone - CII
--IR tablet Dilaudid
--four times daily
--ER tablet Exalgo
--once daily
--opioid tolerant patients
--do not chew or crush
(3) fentanyl - CII
--transdermal delivery system Duragesic
--transmucosal delivery systems
--Actiq fentanyl lozenge
--Fentora - fentanyl buccal tablet
--Abstral - fentanyl sublingual tablet
--Subsys - fentanyl sublingual spray
--intranasal dosage form - Lazanda
(4) codeine - controlled substance schedule variable
--therapeutic categories: analgesic, antitussive
--analgesic - usually in combination with apap (Tylenol #3)
--antitussive usually in combination with guaifenesin
--therapeutic category of guaifenesin - expectorant
--10 mg codeine and 100 mg guaifenesin/5 mL
(5) hydrocodone - CII
--therapeutic categories: analgesic, antitussive
--analgesic, antitussive
--Tussionex (twice daily)
--8 mg chlorpheniramine polistirex/5 mL
--10 mg hydrocodone polistirex/5 mL
--Zohydro ER (twice daily)
--ER hydrocodone capsules
--Hysingla ER (once daily)
--ER hydrocodone tablets
(6) oxymorphone - CII
--Opana
--IR tablet (four times daily)
--Opana ER
ER tablet (twice daily)

55

(7) methadone (Methadose) - CII


--two indications: analgesic, addiction
--pain four times daily
--addiction - once daily
(8) buprenorphine - CIII
--sublingual tablet
--indicated for opioid dependence
--2 mg, 8 mg
--once daily
--parenteral (Buprenex)
--only indicated for pain (four times daily)
--transdermal (Butrans)
--indicated for chronic pain
--5 mcg/hour, 10 mcg/hour, 20 mcg/hour
--10 mcg, 20 mcg in opioid tolerant patients
-- once weekly
--buccal film (Belbuca)
--indicated for chronic pain
--indicated for opioid dependence
--twice daily
(9) buprenorphine, naloxone - CIII
--indicated for opioid dependence
--sublingual tablet
--sublingual film (Suboxone, Bunavail)
--naloxone opioid antagonist
(10) pentazocine, naloxone - CIV
--four times daily
--another opioid antagonist
--naltrexone (Vivitrol) - not controlled substance
--indicated for opioid and alcohol dependence
--injection - once a month
Evzio - naloxone - not controlled substance
--indicated for opioid overdose
--IM injection - auto-injector
(11) butorphanol - CIV
--nasal spray
--four times daily

56

(12) morphine sulfate - CII


--ER tablet
--MS Contin - twice daily
--ER capsule
--Kadian - twice daily
(13) oxycodone - CII
--IR capsule, IR tablet
--four times daily
--Oxaydo - IR tablet
--sodium lauryl sulfate
--IR tablet combination Percocet (oxycodone, apap) - four times daily
--ER tablet
--Oxycontin - twice daily
(14) tramadol - CIV
--IR tablet
--Ultram - four times daily
--Ultracet (tramadol, acetaminophen) - four times daily
--ER tablet
--Ultram ER - once daily
(15)

tapentadol - CII
--IR tablet
--Nucynta - four times daily
--ER tablet
--Nucynta ER - twice daily

--patient counseling:
--take oxymorphone on empty stomach
--no alcohol - from any source - with Kadian
--use tramadol cautiously in patients with seizure disorder
--for all opioids
--somnolence
--avoid alcohol
--constipation
Treatment of opioid-induced constipation:
--Relistor methylnaltrexone
--opioid receptor antagonist - blocks opioid receptors in the intestine
--subcutaneous injection
--every other day
--Movantik - naloxegol
--opioid receptor antagonist - blocks opioid receptors in the intestine
--oral - once daily
57

ANTICONVULSANTS
Generalized seizures (tonic-clonic, absence - petit mal)
Partial seizures (focal seizures)
Anticonvulsant classes:
Barbiturates
--phenobarbital, primidone (Mysoline)
--partial seizures, tonic-clonic seizures
Succinimides
--ethosuximide (Zarontin), methsuximide
--absence seizures
Sulfonamides
--zonisamide (Zonegran)
--partial
Hydantoins
--phenytoin (Dilantin)
--capsule, chewable tablet, oral suspension, parenteral
--ethotoin (Peganone)
--partial, tonic-clonic
--fosphenytoin (Cerebyx)
--parenteral (IV)
--store under refrigeration
--parenteral phenytoin, fosphenytoin are indicated for status epilepticus
Anticonvulsant medications:
carbamazepine (Tegretol, Carbatrol, Epitol)
--partial, tonic-clonic, trigeminal neuralgia, bipolar disorder
--BBWs - agranulocytosis, caution in Asian patients
felbamate (Felbatol)
--partial, Lennox-Gastaut syndrome
--BBWs
--agranulocytosis, hepatotoxicity, bone marrow suppression
lamotrigine (Lamictal)
--partial, tonic-clonic, bipolar disorder, Lennox-Gastaut syndrome
--BBW - serious rashes
gabapentin (Neurontin)
--partial, Restless Legs Syndrome
--pain associated with postherpetic neuralgia (PHN)

58

pregabalin (Lyrica)
--partial, pain associated with PHN, fibromyalgia
--pain associated with diabetic peripheral neuropathy (DPN)
levetiracetam (Keppra)
--partial, tonic-clonic
topiramate (Topamax)
--tablet (Topamax), capsule (Topamax Sprinkle)
--ER capsule (Trokendi XR, Qudexy XR)
--partial, tonic-clonic, Lennox-Gastaut, migraine prophylaxis
divalproex (Depakote)
--partial, absence, bipolar disorder, migraine prophylaxis
--BBW- do not use in pregnancy
oxcarbazepine (Trileptal)
eslicarbazepine (Aptiom)
lacosamide (Vimpat)
--partial
rufinamide (Banzel)
--Lennox-Gastaut Syndrome
vigabatrin Sabril
--two dosage forms - different indications:
--powder for oral solution (West Syndrome)
--tablet (partial seizures in adults)
--BBW - permanent vision loss
Patient counseling for Anticonvulsants:
--decrease effectiveness of hormonal contraceptives
--oral, transdermal, parenteral
--somnolence
--use good dental care with hydantoins (gingival hyperplasia)
--avoid chronic alcohol use with hydantoins
--never suddenly discontinue

59

DEFINITIONS
This self-study guide contains information about generic substitution terminology.
Students are responsible for all the information in this guide.
Generic Substitution - the act of dispensing an unbranded drug product for the drug product
prescribed (i.e. chemically the exact same drug entity in the same dosage form, but
distributed by different companies.)
For example, if a pharmacist receives a new prescription for Ceftin (cefuroxime), he/she may
dispense an unbranded cefuroxime product rather than Ceftin. In other words, the cefuroxime
product dispensed does not have a brand name. Cefuroxime is a second generation
cephalosporin.
Brand name products are protected by patent for 17 years. After this, generics may be
marketed for the brand name product. Generics must be chemically identical to the brand
name product and must also be in the same dosage form and strength as the brand name
product.
Chemical Equivalents (Pharmaceutical equivalents) - two products from different companies
that contain identical active ingredient(s), in identical strengths, in identical dosage forms.
Example: cephalexin 250 mg capsules from Manufacturer A and cephalexin 250 mg capsules from
Manufacturer B are chemical equivalents. The medication is identical, the strengths are identical,
and the dosage forms are identical. The only difference is that the products are from two different
manufacturers (sometimes the term multisource products is used). The terms Chemical
Equivalents and Pharmaceutical Equivalents are synonyms.
Bioequivalents - chemical equivalents that produce similar blood levels.
If the cephalexin capsules in the above illustration produce similar blood levels, they are
bioequivalents. It is assumed that bioequivalents produce similar therapeutic effects.
Nonequivalents-chemical equivalents that do not produce similar blood levels.
Therapeutic Equivalents - chemical equivalents which, when administered in the same dose,
will provide the same therapeutic effect as measured by the control of a symptom or disease.
Therapeutic equivalents are chemical equivalents that produce similar blood levels.
60

ARKANSAS PHARMACISTS CAN SUBSTITUTE THERAPEUTIC EQUIVALENTS.


There are two other ways to consider this:
1.
Arkansas pharmacists can substitute chemical equivalents that produce
similar blood levels.
2.
Arkansas pharmacists can substitute a generic that produces a similar blood
level to the brand name product.
HOW DOES A PHARMACIST KNOW IF A GENERIC PRODUCES SIMILAR BLOOD
LEVELS TO A BRAND NAME PRODUCT?
The pharmacist must refer to the FDA therapeutic equivalence codes for medications. A
therapeutic equivalence code is a two letter code assigned to a medication by the FDA. The first
letter of the code tells the pharmacist whether or not the medication may be substituted. The second
letter provides additional information about the medication such as the dosage form.
The two basic categories into which multisource medications have been placed are:
A drug products considered to be therapeutically equivalent to other
pharmaceutically (chemically) equivalent products and may be substituted.
These medications are chemical equivalents that produce similar blood levels, and therefore
similar therapeutic effects. Pharmacists may substitute A rated generics for the brand name.
Examples of codes in this category are AA, AN, AO, AP, AT, etc.
B drug products not considered to be therapeutically equivalent to other
pharmaceutically (chemically) equivalent products and may not be substituted.
These medications are chemical equivalents but do not produce similar blood levels.
Pharmacists may not substitute B rated generics for the brand name unless approval is
granted from the prescriber. Examples of codes in this category are BC, BD, BR, etc.
Pharmaceutic Alternates - drug products that contain the same therapeutic moiety and
strength, are administered by the same route, but differ in the salt or dosage form. Arkansas
pharmacists cannot substitute pharmaceutic alternates.
Example of Pharmaceutic Alternates:
Bactroban Cream and Bactroban Ointment
These products contain the same therapeutic moiety (mupirocin), strength (2%), and
route of administration (topical), but differ in dosage form.
Therapeutic Alternates - drug products containing different therapeutic moieties (different
generic names) but which are of the same pharmacological and/or therapeutic class and can be
expected to have similar therapeutic effects.
Beta-blocking agents are examples of Therapeutic Alternates. These medications have different
generic names, but are all members of the same medication class.
61

Examples of Beta-blocking agents are:


Bystolic nebivolol
Zebeta bisoprolol
Corgard - nadolol
Tenormin - atenolol
Calcium channel blocking agents are another example of Therapeutic Alternates.
Examples of Calcium Channel Blocking agents are:
Cardizem CD - diltiazem
Procardia - nifedipine
Sular - nisoldipine
Calan verapamil
Therapeutic Substitution - dispensing a therapeutic alternate for the drug product prescribed.
Arkansas pharmacists cannot perform therapeutic substitution.
For example: a pharmacist receives a new prescription for Cardizem CD but is out of stock and
dispenses Sular instead (i.e. dispensing one CCB for another).

62

MEDICATIONS AND PREGNANCY


Administration of a medication to a pregnant patient presents a unique challenge to health care
professionals. In addition to taking maternal pharmacologic mechanisms into consideration, the
unborn child must always be kept in mind as a potential recipient of the medication. Health care
professionals must weigh the benefit of a medication to the mother against its risk to the developing
child. Medications are assigned a Pregnancy Category (A. B, C, D, X) based on their potential for
causing birth defects/harm. A medications Pregnancy Category can change throughout pregnancy.
For example, the Pregnancy Category for meperidine is B during the first and second trimester.
During the third trimester, however, its Pregnancy Category changes to D (designated B/D).
Teratogen - an agent causing abnormal development of an embryo.
Teratogenic medication - a medication causing birth defects.

Pregnancy Category A - controlled studies in women fail to demonstrate a risk to the fetus
in the first trimester (and there is no evidence of risk in later trimesters), and the possibility
of fetal harm appears remote. Examples of Pregnancy Category A medications are
levothyroxine, ferrous sulfate, potassium chloride and multiple vitamins.
Pregnancy Category B - either animal reproduction studies have not demonstrated fetal
risk but there are no controlled studies in pregnant women, or animal reproduction studies
have shown an adverse effect that was not confirmed in controlled studies in women in the
first trimester (and there is no evidence of risk in later trimesters). An example of
Pregnancy Category B medication is insulin.
Pregnancy Category C - either studies in animals have revealed adverse effects on the fetus
and there are no controlled studies in women, or studies in women and animals are not
available. An example of Pregnancy Category C medication is albendazole (Albenza). Albenza
is sometimes prescribed for pinworms (clinical term enterobiasis) however this is not an FDA
approved indication. The therapeutic category of Albenza is anthelmintic.
Pregnancy Category DThere is positive evidence of human fetal risk, but the benefits from
use in pregnant women may be acceptable despite the risk (e.g., if the medication is needed in
a life-threatening situation or for a serious disease for which safer medications cannot be
used). Examples Pregnancy Category D medications are anxiolytic benzodiazepines (alprazolam),
and tetracycline antibiotics (tetracycline, minocycline, doxycycline). Permanent discoloration
(brown-gray) of the teeth may occur if tetracyclines are used during the last half of pregnancy.
Pregnancy Category X--Studies in animals or humans have demonstrated fetal abnormalities
or there is evidence of fetal risk based on human experience. The risk of using the medication
in pregnant women clearly outweighs any possible benefit.
63

Pregnancy Category X medications are contraindicated in pregnant women.


Examples of Pregnancy Category X medications:
a.
isotretinoin
b.
HMG-CoA Reductase Inhibitors
c.
misoprostol
d.
oral contraceptives
e.
warfarin sodium
f.
hypnotic benzodiazepines (temazepam)
g.
methotrexate
h.
thalidomide-Thalomid
In the early 1960s, thalidomide was widely prescribed to women in their first trimester of
pregnancy for the treatment of morning sickness. Unfortunately the medication caused limb
defects (clinical term - phocomelia) in thousands of infants before the cause and effect
relationship between thalidomide and birth defects was recognized. As a result of this
tragedy, thalidomide was removed from the market for many years. Today thalidomide is
once again available under the trade name Thalomid. Thalomid is indicated for erythema
nodosum leprosum, a severe and debilitating condition associated with leprosy.

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