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prodrug

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1. Generic Name: Aspirin
Pharmacologic class: ANTT-THROMBOTIC AGENT
Drug formulation: TABLET 80 mg
Mechanism of Action: INHIBITS PROSTAGLANDIN RELEASE; inhibits more COX 1 than
COX 2
Indication: For ischemic stroke, MI
Dose: Adult: Ischemic stroke- 50- 325 mg initial; Angina 75-300 mg od; Secondary Prevention
for 75-325 mg od
Contraindications: Hypersensitivity to Aspirin, Asthma and rhinitis, avoid in children with
viral infection w/ or w/o fever can cause REYE’S SYNDROME
Interactions:
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Beta blockers
ACE
Acetazolamide increase concentration
Diuretics diminish diuretics effect
Methotrexate inhibit renal clearance
Adverse reactions:
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Fever, hypothermia
Dehydration, metabolic acidosis
Nausea and Vomiting
Rhabdomyolysis
2. Generic name: Bambuterol
Pharmacologic class: B2-adrenoceptor agonist
Drug formulation: Oral 1o mg tablet/ 1mg/ 60 ml oral solution
Mechanism of Action: relaxes bronchial smooth muscle by acting to B2-receptors
Indication: Persistent reversible airway obstruction
Dose: Adult: 10-20 mg od
Children: 2-5 yrs old 10 mg in general ; 5mg Asian children
10 mg initial dose
Warning/Precautions: Can cause hypokalemia, monitor K levels; Used in precaution for
lactating and pregnant women
Adverse reactions: tremor, headache
3. Generic Name: Dipivefrine
Pharmacologic class: prodrug for epinephrine
Drug formulation: Ophthalmic solution
Indication: open angle glaucoma
Dose: Adult: instill 1 drop every 12 hours
4. Generic name: Valganciclovir
Pharmacologic class: Antiviral ; Prodrug for ganciclovir
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Drug formulation: Tablet 450 mg, oral solution
Indication: For CMC cytomegalovirus retinitis
Dose: Adult: CMC rhinitis 900 mg per day
Children: 4 months to 16 yrs old = 7 x BSA x Cr Cl
Warning/Precautions: Do not give to pregnant women, it is teratogenic
5. Generic name: Secnidazole
Pharmacologic class: Nitro imidazole antibacterial drug
Indication: Bacterial vaginosis; Trichominiasis; Candidiasis
Dose: Adult: 2 g orally once a day
Contraindications: Hypersensitive to secnidazole
Warning/Precautions: Can cause vaginal yeast infection; Do not breastfeed
Interactions: interacts with ethanol
Adverse reactions: Nausea and vomiting ; headache
6. Generic name: Latanoprost
Pharmacologic class: Prostaglandin analog
Mechanism of Action: ester pro drug to free acid; analog to F2 alpha prostraglandins
Indication: Open angle glaucoma; Ocular hypertension
Dose: Adult: Lower intraocular pressure, instill 1 drop
Adverse reactions: Iris pigmentation changes, Intraocular inflammation
7. Sulfasalazine
Pharmacologic class: DMARDS; Disease Modifying Antirheumatic Drugs
Drug formulation: Suppository
Mechanism of Action: direct anti-inflammatory action in the colon
Indication: IBD; Inflammatory Bowel Disease; Rheumatoid Arthritis
Contraindications: Hypersensitivity to Sulfa drugs; Blood dyscrasias
Warning/Precautions: Hepatic/ renal impairments; G6PD deficient ; - hemolytic anemia
8. Olsalazine
Pharmacologic class: Prodrug for Mesalamine; Anti-inflammatory
Drug formulation: Capsule
Mechanism of Action: Derivative of salicylic acid; it is converted by the bacteria in the colon to
mesalamine
Indication: treatment of Inflammatory Bowel Disease and Ulcerative Colitis
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9. Enalapril
Pharmacologic class: ACE inhibitors; Converted to Enalaprilat
Mechanism of Action: Pro drug for enalaprilat; inhibits angiotensin converting enzyme
Indication: Management of hypertension, monotherapy or in combination
Dose: Adult: IV solution; 1.25 mg every 6 hrs; Oral 5 mg od
Children: 20 – 50 kg; 2.5 mg od above 50 kg; 5 mg od
Contraindications: History of angioedema with ACE Inhitors; not for pregnant women
Warning/Precautions: Cerebrovascular disease
Interactions: Potentiate with hypotensive with other hypertensive drug
Adverse reactions: Chest pain, angina pectoris, tachycardia, orthostatic hypertension
10.
Chloramphenicol succinate
Pharmacologic class: Anti-infectives
Drug formulation: Otic and Opthalmic drops, IV solution; Eye ointment
Mechanism of Action: Antibiotic, eye and ear infection, typhoid fever;
Contraindications: Hypersensitivity to chloramphenicol, blood dyscrasias, Pregnancy and
lactation
Warning/Precautions: Avoid prolong use, not for prophylactic use
Interactions: Enhances coumarin effects, antiepileptics,
Adverse reactions: Ototoxicity, eye disorder, optic neuritis, N and V, stomatitis
11.
Simvastatin
Pharmacologic class: Statin; HMG co-reductase inhibitors; Prodrug that hydrolyzed its lactone
ring into B-deta-hihyroxy acid
Contraindications: Pregnancy and lactation
Interactions: Increased myopathy and rhabdomyolysis with amiodarone;
12. Famciclovir
Pharmacologic class: Antiviral; Pro drug to the active anti-viral compound penciclovir
Drug formulation: Oral dosage dorm
Indication: acute herpes zoster infections shingles
Dose: Adult: herpes zoster infections shingles 500 mg tid for 7 days
Adverse reactions: Headache, nausea and vomiting, constipation; dyspepsia
13. Paracetamol
Pharmacologic class: Analgesic
Drug formulation: Tablet, Syrup
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Drug’s chemical structure:
Interactions: Adverse reactions: Allergic reactions , flushing
14. Sulindac
Pharmacologic class: NSAIDS
Drug formulation: Tablet
Mechanism of Action: converted to active sulfide compound by liver enzymes; inhibit
prostaglandin release
Interactions: nephrotoxicity with ciclosporine
Adverse reactions: HA, N and V, diarrhea, rash, urine discolaration
15. IBUPROFEN
Pharmacologic class: NSAIDS
Drug formulation: Tablet
16. Azathioprine
Pharmacologic class: Immunosuppressants; Prodrug for 6-Mercapturine
Indication: Adjunct to prevent organ rejections
17. Omeprazole
Pharmacologic class: Proton Pump Inhibitor
Drug formulation: Tablet; IV solution
Mechanism of Action: blocks final step in gastric secretion
Indication: Eradication of Helicobacter pylori; Duodenal and gastric ulcer; GERD
Adverse reactions: Hypomagnesimia, SLE, Clostridum difficili diarrhea
18. Allopurinol
Pharmacologic class: Xanthine oxidase inhibitor
Drug formulation: Tablet
Mechanism of Action: A produg that is converted to oxypurinol
Indication: Gout, hyperuricemia
19. Terfenadine
Pharmacologic class: Metabolized into Fexofenadine ; Antihistamine
Drug formulation: Tablet
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20. Codeine
Pharmacologic class: Opioid Analgesic; converted to morphine (active metabolite)
Mechanism of Action: phenantherene derivative; suppress cough
Indication: IM moderate pain- 30- 60 mg every hour as needed
Adverse reactions: CNS depressions; blood and lymphatic system disorders
21. Disulfiram
Pharmacologic class: Alcohol antagonist
Drug formulation: Tablet
Drug’s chemical structure: blocks alcohol oxidation
Contraindications: Alcohol containing products
22. Pyridoxine
Pharmacologic class: Vitamin B6 derivative; converted to pyridoxal 5-phosphate
23. Isoniazid
Pharmacologic class: Anti tuberculosis
Drug formulation: Tablet, Oral Solution, Solution for Injection
Mechanism of Action: activated by bacterial catalase;
Indication: to treat active tuberculosis;
Contraindications: Hypersensitivity to the drug
Warning/Precautions: History of psychosis, neuropathy, pyridoxine neuropathy
Interactions: (-) hepatic metabolism of benzodiazepine; increase toxicity warfarin;
Adverse reactions: optic neuritis; peripheral neuritis;
24. Tegafur
Pharmacologic class: Anti-metabolites; Anti neoplastic
Mechanism of Action: Prodrug of 5-fluorouracil; used for colon/bowel cancer
Dose: Children: not applicable
Contraindications: Pregnancy/ lactation
Warning/Precautions: hepatic impairment
Interactions: Increase phenytoin toxicity; Increase thrombosis for tamoxifen
Adverse reactions: N & V, mucositis; alopecia; myocardial ischemia
25. Fosinopril
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Pharmacologic class: Ace inhibitors
Mechanism of Action: Prodrug for Fosinoprilat
Indication: Mild to moderate hypertension,
Dose: Adult: 10 mg od; risk of hypotension 5 mg od; maintenance 10-40 mg once daily
Children: based on weight;
Contraindications: history of angioedema with ACEis; pregnancy/ lactation
Warning/Precautions: Mitral valve stenosis/ Dialysis/ renal impairment
Interactions: Increase lithium toxicity;
Adverse reactions: Persistent and nonproductive COUGH; URTI infection, N and V; Fatal:
anaphylaxis
26.
Naproxen
Pharmacologic class: NSAIDS
Indication: Arthritis; osteoarthritis; dysmenorrhea
Dose: Adult:
Children: based on weight
Contraindications: Contraindicated to known hypersensitivity to naproxen
Adverse reactions: cardiovascular risk; GIT discomfort; diarrhea; headache, hypersensitivity
reaction
27. Levodopa
Pharmacologic class: Antiparkinsons drug
Drug formulation: tablet
Mechanism of Action: converted into dopamine
Indication: symptoms of Parkinsonisms;
Dose: Adult: 250 mg 2 to 4 times a day, not more 8 g a day
Children:
Contraindications: Psychotic patients exacerbation to mental disturbance, may activate
malignant melanoma
Warning/Precautions: open-angle glaucoma; high blood pressure, asthma, COPD; ulcers,
depression, psychosis
Interactions: Pyridoxine, MAOi inhibitors
Adverse reactions: Anxiety, confusions, delusions, anorexia,, N and V ;
28. Ramipril
Pharmacologic class: ACEis; active metabolite Ramiprilat
Drug formulation: Capsule/ Tablet
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Mechanism of Action: (-) ACE ; result to blood pressure decreases
Indication: - hypertension, prevention heart failure, MI
Dose: Adult: 2.5mg once a day; preventing heart attack 2.5 mg once a day;
Children: not applicable
Contraindications: Renal artery stenosis, low blood pressure
Warning/Precautions: Can cause to serious harm to the baby; do not use in pregnancy
Adverse reactions: Can cause dizziness, tiredness, causes dry cough
29.
Pentazocine
Pharmacologic class: Analgesics
30. Fludarabine
Pharmacologic class: Antimetabolites; purine nucleoside
Mechanism of Action: A prodrug that is converted to the free nucleoside 9-beta-D-arabinosyl-2fluroadenine
Indication: leukemia and lymphoma
Dose: Adult: leukemia;
Children:
Contraindications: Hemolytic anemia; lactation
Warning/Precautions: Sever impairment of bone marrow; hepatic impairment; pregnancy
Adverse reactions: Skin cancer exacerbations, seizure, peripheral neuropathy; GI: N and V,
diarrhea; GI bleeding, constipation Respiratory: cough, bronchitis, hypoxia
31. Benzhydrocodone
Mechanism of Action: Prodrug for hydrocodone;
Contraindications: Bronchial asthma; GI obstruction
Warning/Precautions: can cause drowsiness and breathing problems when taken with alcohol
Adverse reactions: N and V, headache, drowsiness
32. Bacaillin
Pharmacologic class: Penicilllins
Drug formulation: Oral tablets/ capsule
Mechanism of Action: prodrug of ampicillin;
Indication: pneumonia; typhoid fever, UTI
Dose: Adult:400 mg
Children:
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Contraindications: hypersensitivity to Penicillins
Interactions: Probenecid stays longer
Adverse reactions: hypersensitivity reactions urticaria, angioedema, serum sickness,
thromcytopenia
33. Temozolomide
Mechanism of Action: hydrolyzed to 3-methyl-imidazole-4 carboxamide active metabolite to
dacarbazine
Indication: treatment recurrent or progressive gliomas, melanoma
Dose: Adult: 200 mg/m2 ; 150mg/ m2
Children:
Contraindications: Hypersensitivity to dacarbazine;
Warning/Precautions: Sever hepatic/ renal impairment; avoid becoming pregnant; irreversible
infertility
Interactions: reduce effectiveness of vaccines;
Adverse reactions: N and V; diarrhea; stomatitis; tremors, speech disorder;
34. Capecitabine
Pharmacologic class: Antineoplastic,
Drug formulation: Tablet
Mechanism of Action: Active metabolite fluorouracil;
Indication: first line treatment for colorectal carcicnoma;
Contraindications: altered
Interactions: increase plasma concentration of phenytoin;
Adverse reactions: N and vomiting, palmar plantar; fatigue
35. Fosphenytoin
Pharmacologic class: Anti-seizure drug
Drug formulation: IV solution
Mechanism of Action: converted to phenytoin;
Contraindications: Hypersensitivity to phenytoin;
Warning/Precautions: hypotension, sever myocardial insufficiency, hyperbilirubinemia;
phosphate restrictions; poor and intermediate metabolizers
Interactions: increase plasma levels amiodarone, azole antifungals;
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36. Prednisone
Pharmacologic class: Corticosteroids
Drug formulation: Oral solution
Mechanism of Action: converted into prednisolone
Indication: Inflammation; rheumatoid arthritis;
Warning/Precautions: hypertension, osteoporosis,
Interactions: antiplatelet drug such as clopidogrel,
Adverse reactions: acne, heart burn, irregular menstrual period
37. Pivampicillin
Pharmacologic class: Antibacterial
Mechanism of Action: Prodrug of ampicillin
Contraindications: Porphyria;
Warning/Precautions: Neurotoxicity
Adverse reactions: fever, rashes, angioedema;
38. Selexipag
Pharmacologic class: Selective prostacyclin receptor agonist
Mechanism of Action: Prodrug of ACT-333679 (the free carboxylic acid)
Indication: treatment of pulmonary arterial hypertension
Contraindications: Severe hepatic impairment;
Adverse reactions: headache, diarrhea,
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