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(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
1
(5) fluoroquinolones
--ciprofloxacin
--moxifloxacin (Avelox)
levofloxacin (Levaquin)
gemifloxacin (Factive)
(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
3
(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
5
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
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
10
11
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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ISOTRETINOIN
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
13
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
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.
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.
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.
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.
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
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.
3.
4.
flunisolide
5.
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
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
naproxen (Naprosyn)
piroxicam (Feldene)
diclofenac potassium
meloxicam (Mobic)
indomethacin
oxaprozin
ketoprofen
cell membranes
arachidonic acid
cyclooxygenase -1
cytoprotective prostaglandins
cyclooxygenase-2
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
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
29
ANTIVIRAL AGENTS
--acyclovir - Zovirax
--famciclovir - Famvir
--valacyclovir - Valtrex
--valacyclovir is converted to acyclovir
--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
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fesoterodine (Toviaz)
ANTIFUNGALS
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
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
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
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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
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
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 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
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)
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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)
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
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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)
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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.
6.
51
tricyclics
amitriptyline
clomipramine [Anafranil (only indicated for OCD)]
doxepin [Silenor (only indicated for insomnia)]
desipramine (Norpramin)
imipramine (Tofranil)
nortriptyline (Pamelor)
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
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)
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56
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)
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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
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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.
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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.
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