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Pharmaceutical preparations are applied topically to the eye to treat surface or intraocular conditions, including bacterial,

fungal, and viral infections of the eye or eyelids; allergic or infectious conjunctivitis or inflammation; elevated intraocul ar
pressure and glaucoma; and dry eye due to inadequate production of fluids bathing the eye.
The normal volume of tear fluid in the cul-de-sac of the human eye is about 7-8 microliter.

Pharmacologic categories of ophthalmic drugs:

Anesthetics: Topical anesthetics, such as tetracaine, cocaine, and proparacaine, are employed to provide pain relief
preoperatively, postoperatively, for ophthalmic trauma, and during opthalmic examination.
Antibiotic and antimicrobial agents: Used systematically and locally to combat ophthalmic infection. Among the agents
topically are azithromycin, gentamicin sulfate, sodium sulfacetamide, ciprofloxacin hydrochloride, ofloxacin, polymyxin B-
bacitracin, and tobramycin.
Antifungal agents: Among the agents used topically against fungal endophthalmitis and fungal keratitis are amphotericin
B, natanmycin, and flucytosine.
Anti-inflammatory agents: Used to treat inflammation of the eye, as allergic conjunctivitis. Among the topical anti-
inflammatory steroidal agents are flourometholone, prednisolone, and dexamethasone salts. Nonsteroidal anti-inflammatory
agents include diclofenac, flurbiprofen, ketorolac, and suprofen.
Antiviral agents: Used against viral infections, as that caused by herpes simplex virus. Among the antiviral agents used
topically are trifluridine, ganciclovir, and vidarabine.
Astringents: Used in the treatment of conjunctivitis. Zinc sulfate is a commonly used astringent in ophthalmic solutions.
Beta-adrenergic blocking agents: Agents such as betaxolol hydrocholride, levobunolol hydrochloride, metipranolol
hydrochloride, and timolol maleate are used topically in the treatment of intraocular pressure and chronic open-angle
glaucoma.
Miotics and other glaucoma agents: Used in the treatment of glaucoma, accommodative esotropia, convergent
strabismus, and for local treatment of myasthenia gravis. Among the miotics are pilocarpine, echothiophate iodide, and
demecarium bromide.
Mydriatics and Cycloplegics: Mydriatics allows examination of fundus by dilating pupil. Mydriatics having a long duration
of action are termed cycloplegics. Examples are atropine, scopolamine, homatropine, cyclopentolate, phenylephrine,
hydroxyamphetamine, and tropicamide.
Protectants and Artificial tears: Solutions employed as artificial tears or as contact lens fluids to lubricate the eye
contain agents such as carboxymethyl cellulose, methylcellulose, hydroxypropyl methylcellulose, and polyvinyl alcohol.
Vasoconstrictors and Ocular Decongestants: Vasoconstrictors applied topically to the mucous membranes of the eye
cause transient constriction of the conjunctival blood vessels. They are intended to soothe, refresh, and remove, redness
due to minor eye irritation.
Examples are naphazoline, oxymethazoline, and tetrahydrozoline hydrochlorides.

Pharmaceutical Requirements:

Sterility and Preservation : it is preferable to sterilize ophthalmics in their final containers by autoclaving at 121 degrees
Celsius for 15 minutes. Examples of antimicrobial preservatives are benzalkonium chloride, 0.004% to 0.01%.
Isotonicity Value: The term Isotonic, meaning equal tone, is commonly used interchangeably with isomotic.
Buffering: The pH of an ophthalmic preparation and buffered for one more of the following purposes:
A. for greater comfort to the eye
B. to render the formulation more stable.
C. to enhance the aqueous solubility of the drug,
D.To enhance the drugs bioavailabity.
E. To maximize preservative efficacy.
Viscosity and Thickening agents: Viscosity is a property of liquids related to the resistant flow.
Ocular Bioavailability: Is an important factor in the effectiveness of an applied medication.

Packaging Ophthalmic Solutions and Suspensions

A few commercial ophthalmic solutions and suspensions are packaged in small glass bottles with separate glass or plastic
droppers, most are packaged in soft plastic containers with a fixed built-in dropper. Ophthalmic solutions used as
eyewashes are generally packed with an eye cup, which should be cleaned and dried thoroughly before each use.
RADIOPHARMACEUTICALS

-have been defined as radioactive drugs that, when used for the purpose of diagnosis or therapy, typically elicit no
physiological response from the patient. This definition is strongly supported by the Nuclear Medicine community's collective
experience in administering radiopharmaceuticals: most practitioners, in their entire careers, have not observed a
physiological response or an adverse reaction following administration of a radiopharmaceutical.

The USP 30-NF 25 lists 77 official radioactive pharmaceuticals
The following describes some of the radiopharmaceuticals frequently used in daily practice.
Other radiopharmaceuticals are being used for the delivery of MABs and biotechnologic drugs.
MABs -Monoclonal Antibodies


Some radioactive pharmaceuticals

-Technetium-99M(99MTC) -Rhenium-186(186Re)
-Strontium-89 Chloride(89Sr) & Rhenium-188(188Re)
-Yttrium-90(90Y) -188Rhenium-HEDP
-Thallous-201 Chloride(201Tl) -Lutetium-177(177Lu)
-Gallium-67 Citrate (67Ga) -Holmium-166(166Ho)
-Indium-111 Chloride(111In) -Samarium-153(153Sm)
-Sodium Iodide-123(123I) -Sodium Iodide-131(131I)


Technetium-99M (99MTc)

-possesses a relatively short half-life of 6 hours, which allows administration of activity for faster and clearer images
-it provides low radiation dosimetry and highly efficient detection of photons by planar scintography.
-99mTc sulfur colloid is used for imaging areas of functioning reticuloendothelial(RE) cells in the liver, spleen and bone
marrow
-and also used as other diagnosing purposes imaging of lympatic vessels and nodes draining.
-99mTc-DPTA(diethylenetriaminepentaacetic acids; pentetate), is preferred for use of cerebrospinal fluid procedures that
require shorter imaging times.


Strontium-89 Chloride (89Sr)
- Metastron is a sterile, non pyrogenic aqueous solution for intravenous use and contains no preservative.
-it decays by beta emission, with a physical half life of 51 days. ; the beta emission is vey harmful to skeletal tissue and its
clinical use is reserved for bone pain palliation associated with primary bone tumors and metastatic involvement (blastic
lesions)
-the uptake of 89Sr by bone occurs preferentially in sites of osteogenesis imferfecta- a condition where the formation of
brittle bones prone to fractures.
Yttrium-90(90Y)
-a trivalent radioactive metal, is a pure beta-emitting radionuclide.it possesses a physical half life of 64.2 hours (2.68 days)
-is frequently used in human studies, in part because of its routine availability from commercial vendors as a
sterile,pyrogen-free products with high specificity 15.
-its principal therapeutic application is in solid large tumors and lymphomas ;in addition it is employed in pain palliation with
soft tissue.
-TheraSphere is a therapeutic device used in patients with liver cancer
Thallous-201 Chloride(201Tl)
-is available as a sterile, isotonic nonpyrogenic solution for intravenous administration
-has a physical half-life of 73.1 hours and decays by electron capture to mercury 201Hg.
-And also be used as an adjunct to the diagnosis of ischemic heart disease
-201Tl has its most important use is in the diagnosis and monitoring of Pneumocystis carinii of AIDS.
Gallium-67 Citrate(67Ga)
-is available as a sterile, pyrogen-free aqueous solution. Chemically this drug behaves similarly to ferric ion (Fe+3) and
demonstrate a half-life of 78 hours.
-it can localize certain viable primary and metastatic tumors and in focal sites of infections.
-it may be useful in demonstrating the presence and extent of malignancies associated with Hodgkin disease, lymphomas
and bronchogenic carcinoma.
-its important use is in the diagnosis and monitoring of Pneumonia carinii of AIDS and used as a diagnostic screen in cases
of prolonged fever.
Indium-111 Chloride(111In)
-has become a popular radionuclide as a label for MABs
-It has a long half-life, which allows multiple images to be taken up to 10 to 14 days after administration.
-it has dual peaks provides superior planar images because it lacks beta emission, it can administered in rather high doses.
-Capromab penditide (ProstaScint) is a MAB imaging agent that is linked to 111In, these drug seeks out and attaches itself
to prostate cancer and its metastases.
-it can aid management by helping identify when the cancer has metastasized from the prostate bed to regional lymph
nodes and as a diagnostic imaging agent in post prostatectomy.
Sodium Iodide-123(123I)
-is available as an oral capsule and is generally preferable to 131I because it delivers lower radiation doses and has better
imaging properties
-it is used diagnostically to evaluate thyroid function and morphology.
-it emits only gamma rays. About 5% to 30% administered dose is concentrated in the thyroid gland at 24 hours; And has
an effective half-life of 13 hours, and the remaining administered activity is distributed within the extracellular fluid and has
an effective half life of 8 hours.
Sodium Iodide-131(131I)
-is available as a volatile solution that can be purchased from a manufacturer by a nuclear pharmacist into an oral capsule
or solution.
-it is used for thyroid function studies by determining the fraction of administered radioiodine activity taken up by the
thyroid gland.
-the beta emission from the 131I destroys thyroid tissue and in small amounts, can be used for diagnostic thyroid imaging.
-has a half-life of 8 days.
Samarium-153(153Sm)
-has a short half-life of 1.9 days, which can be advantageous for administering repeated doses
-it is a low energy beta emitter which is advantageous for treating small clusters of tumorous cells.
-it is chelated with ehtylenediamine tetramethylene phosphonate (153Sm-EDTMP, Quadramet) for the relief of pain in
patients with osteoblastic metastatic bone lesions that enhance radionuclide bone scan.
-its MABs are being used in animal research to study angiogenesis, the development of new blood vessels.

Holmium-166(166Ho)
-complexed with 166Ho-DOTMP has demonstrated potential to treat multiple myeloma and to ablate bone marrow.
-it can be used for eradication of multiple mycloma cells and normal stem cells.
-166Ho in ferric hydroxide macroaggregate complex (166Ho-FHMA) shown to provide beneficial outcomes for equine
metacarpophalangeal and metatarsophalangeal.
Lutetium-177(177Lu)
-is a rare earth metal with a physical half-life of 6.75 days
-it is being investigated in more than 30 clinical applications, including treatment of some types of cancer ; colon, ovary and
lung cancer.
-its radiation energy will be absorbed in very small tumors and micro metastases.
Rhenium-186(186Re) &
Rhenium-188(188Re)
-are important radionuclides with therapeutic potential.
-186Re has a higher beta particle energy and shorter half-life than 188Re.
-188Re is generally more appropriate for larger tumors targeting and possesses a reasonably fast clearance from the blood
and nontarget tissue.
-186Re is a medium beta particle emitter with a 3.7 day half-life which is more appropriate use with biomolecules that are
not cleared from the bloodstream very rapidly.

188Rhenium-HEDP (Hydroxyl Ethylene Diphosphonate)
-is a new radiopharmaceutical for the treatment of metastatic bone pain.
-has a short physical half-life of 16.9 hours
-one study demonstrated a maximum decrease in metastatic bone pain from the third to eight eighth week, week after
therapy initiation.

Bacterial Vaccines
v A vaccine is suspension of attenuated (live) or inactivated (killed) microorganism or fractions thereof that are
administered to induce immunity and prevent disease.
v The organism is grown in a suitable broth medium in a controlled environment of temperature, ph, and oxygen tension.
v A live attenuated vaccine can also be produced by genetic alternation of the pathogenic organism.
v The organism is incapable by reverting to its more pathogenic form
Viral Vaccines
v The final viral product may contain a single immunogen (monovalent) or multiple immunogens (polyvalent) to elicit
immunity against the same disease.
v The vaccines is may remain as the whole virion or be further chemically processed to split into subvirion vaccine as is the
case with theinfluenza virus vaccine.
v This virus is prepared with three virus strain. Since 1977, Influenza A (H1N1), (H3N2) and influenza B viruses has
circulated globally.
v Vaccination with the trivalent influenza vaccine continues to be recommended because the vaccine can provided partial
protection against related strains and reduce the risk for influenza-related complications and deaths.
v It was strongly recommended annually for children aged 6 months or more with certain risk factor, including but not
limited to asthma, cardiac disease, sickle cell disease.
v Gene therapy- allows the DNA template to be placed within a cell, transcribed into messenger RNA, and expressed as a
costimulatory protein.
Toxoids
v Bacteria are propagated, and after the required growth is achieved, the culture is filtered through a sterilizing membrane
filter.
v The filtrate that contains the toxin (exotoxin) is then processed.
v The detoxified toxin (toxoid) may be plain or contain and adjuvant (e.g., alum, aluminium hydroxide, aluminium sulfate).
Human Immune Sera and globulins
v Human Immune Sera or homologous Sera, include immunologlobin and hyperimmune sera for specific diseases.
v These contain the specific antibodies obtain from the blood of humans and produced as a result of having had specific
disease or having been immunized against it with a specific biologic product.
v The source of homologous sera is the pooled plasma of adult donors
v The pooled plasma of adult donor must be free of hepatitis B antigen and antibodies to HIV.
v Sera have the greatest value for the treatment of acute disease, although they are also useful in some instance to
prevent illness when immediate protection is needed.
Animal Immune Sera (Heterogonous Sera)
v Immune sera are by immunization of horses against the specific immunogens. (e.g., toxin, venom).
v Plasma is harvested, it is separated by fractional precipitation into two components: immunologically active
(immunoglobulin) and immunologically inactive ( albumins, Clothing factor) ones .
v The immunologically active component is treated with pepsin to remove the complement-activating components of the
molecules and render it less immunogenic.
v This category of Pharmaceutical includes antitoxin and antivenins.
v Antitoxin are produced by inoculating horses with increasing doses of the toxoids and exotoxins.
v Antivenins are produced similarity, by inoculating horses with the venom of selected species and harvesting the plasma.

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