1
COX INHIBITORS, RHEUMATOID ARTHRITIS AND OSTEO DRUGS
Cyclooxygenase Inhibitors: Nonsteroidal Anti-inflammatory Drugs and Acetaminophen
Aspirin [acetylsalicylic acid, ASA, etc.]
Fun. Class: Nonopioid analgesic, nonsteroidal anti-inflammatory, antipyretic, antiplatelet
Chem. Class: Salicylate
Available OTC
Actions: Decreases inflammation/pain/fever by inhibiting COX-2 irreversibly. Duration of action depends on
how quickly specific tissues can synthesize new molecules of COX1/2. Protects from MI/Ischemic stroke by
inhibiting COX-1.
Uses: mild to moderate pain or fever (including rheumatoid arthritis), suppression of inflammation,
analgesia, reduction of fever, dysmenorrhea, suppression of platelet aggregation, cancer prevention
Side/Adverse Effects: Stomach ulcers, bleeding, renal impairment. Gastrointestinal distress, heartburn, and
nausea. Occult GI bleeding occurs often (usually insignificant), contraindicated with bleeding disorders, with
HTN – increased risk of hemorrhagic stroke (but protects against ischemic stroke). Reversible renal
impairment, Salicylism when levels slightly more than therapeutic (tinnitus, sweating, headache, dizziness).
Reye’s syndrome in children (encephalopathy, fatty liver degeneration). Pregnancy category D.
Acetaminophen [Tylenol, Paracetamol, etc.]
Func. class: Nonopioid analgesic, antipyretic
Chem. class: Nonsalicylate, paraaminophenol derivative
Available OTC
Actions: analgesic/antipyretic (reduces fever). Blocks pain impulses peripherally that occur in response to
inhibition of prostaglandin synthesis, does not possess anti-inflammatory properties/rheumatic. No
inhibition of platelet aggregation/ GI ulcers? Kidney impairment
Uses: mild to moderate pain or fever, headache (migraine), dysmenorrhea, osteoarthritis.
Side/Adverse Effects: no Reye’s. Stevens-Johnson (toxic epidermal necrolysis), may cause hypertension,
asthma association? Risk of bleeding with warfarin? Excessive use of EtOH likely to damage liver if also used
with excessive acetaminophen use (hepatotoxicity), deadly in overdose (Rx with acetylcysteine, which is
also used with COPD), hypersensitivity/anaphylaxis with aspirin excess.
Celecoxib [CeleBREX]
Fun. Class: Nonsteroidal anti-inflammatory, antirheumatic
Chem. Class: COX-2 inhibitor
Actions: inhibits prostaglandin synthesis by selectively inhibiting COX-2, an enzyme needed for biosynthesis.
Decrease pain/inflammation/no GI SEs.
Uses: Acute, chronic rheumatoid arthritis (symptomatic relief, DMARDs), acute pain, primary
dysmenorrhea.
Side/Adverse Effects: Safer than conventional NSAIDS short term? GI ulcers [high alert drug], MI/Stroke
(vasoconstriction, doesn’t inhibit platelet aggregation), Cardiovascular (e.g. HTN, peripheral edema),
impairs renal functions. Last choice drug in long term pain control.
Ibuprofen [Advil, etc.]
Available OTC
Fun. Class: NSAID
Chem. Class: Propionic acid derivative
Actions: Inhibits reversibly COX-1/COX-2 by blocking arachidonate, analgesic, ant inflammatory, antipyretic
Uses: pain, fever, migraine, dysmenorrhea, arthritis.
Side/Adverse Effects: gastric bleed/ulcers, impair kidney, teratogenic?
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Drug Therapy of Rheumatoid Arthritis
Etanercept [Enbrel]
Func. class: Antirheumatic agent
Chem. class: Anti-TNF agent
Actions: DMARDs (Disease modifying antirheumatic drugs)via recombinant DNA technology;
immunosuppressive: target specific components of inflammatory process that can injure joints; interacts
with GABA receptors.
Uses:
Side/Adverse Effects: injection-site reactions, infections (e.g. TB), Stevens-Johnson/toxic epidermal
necrolysis (TEN), heart failure, malignancies, CNS demyelination (e.g. MS), aplastic anemia.
Celecoxib [CeleBREX]
Fun. Class: Nonsteroidal anti-inflammatory, antirheumatic
Chem. Class: COX-2 inhibitor
Actions: inhibits prostaglandin synthesis by selectively inhibiting COX-2, an enzyme needed for biosynthesis.
Decrease pain/inflammation/no GI SEs.
Uses: Acute, chronic rheumatoid arthritis, acute pain, primary dysmenorrhea.
Side/Adverse Effects: Safer than conventional NSAIDS short term? GI ulcers [high alert drug], MI/Stroke
(vasoconstriction, doesn’t inhibit platelet aggregation), Cardiovascular (e.g. HTN, peripheral edema), impairs
renal functions. Last choice drug in long term pain control.
Methotrexate [Metoject, etc.]
Func. class: antineoplastic-antimetabolite (vesicant)
Chem. class: Folic acid antagonist
Actions: Inhibits an enzyme that reduces folic acid, which is needed for nucleic acid synthesis in all cells;
specific to S phase of cell cycle; immunosuppressive from decreased B/T lymphocyte activity.
Uses: RA, others.
Side/Adverse Effects: hepatic fibrosis, bone marrow suppression, GI ulcerations, pneumonitis. Category X in
pregnancy, life expectancy decreases (CV disease, infection, certain cancers).
Sulfasalazine [Salazopyrin]
Fun. Class: GI anti-inflammatory, antirheumatic (DMARD)
Chem. Class: Sulfonamide
Actions: anti-inflammatory and immunomodulatory
Uses: RA
Side/Adverse Effects: NVD/anorexia/pain, pruritus, rash, urticaria.
3
Drugs Affecting Calcium Levels and Bone Mineralization
alendronate [Fosamax]
Func. class: Bone-resorption inhibitor
Chem. class: Bisphosphonate
Actions: Decreases the rate of bone resorption and may directly block dissolution of hydroxyapatite crystals
of bone, inhibits osteoclast activity. Inhibits osteoporosis/bone resorption.
Uses: osteoporosis, glucocorticoid-caused osteoporosis, Paget’s, hypercalcemia/bone Mets in cancer.
Side/Adverse Effects: serious SE (e.g. eye inflammation, jaw necrosis, AF)
Calcitonin [Caltine, Calcimar]
Fun. Class: Parathyroid agents (calcium regulator)
Chem. Class: polypeptide hormone
Actions: decreases bone reabsorption, blood calcium levels; increases deposits if calcium in bones; opposes
parathyroid hormone.
Uses: Paget’s disease, osteoporosis, hypercalcemia.
Side/Adverse Effects: none listed
Cinacalcet [Sensipar]
Func. class: Calcium receptor agonist
Chem. class: polypeptide hormone
Actions: directly lowers PTH levels by increasing sensitivity of calcium-sensing receptors to extracellular
calcium. Fools parathyroid glands into decreasing production of PTH by amplifying ability of Ca 2+ to
negatively feedback on parathyroid glands PTH production.
Uses: hypercalcemia with parathyroid carcinoma, hyperparathyroidism.
Side/Adverse Effects: none listed.
Denosumab [Prolia, Xgeva]
Func. class: Bone resorption inhibitor
Chem. class: Monoclonal antibody, bone resorption
Actions: 1st in class osteoclast inhibitor. Monoclonal antibody
Uses: osteoporosis in M and postmenopausal F with high fracture risk, bone loss with certain anti-CA Rx,
prevention of bone fracture, spinal cord compression, bone pain from bone metastases from solid tumors.
Side/Adverse Effects: hypocalcaemia, infections, jaw osteonecrosis.
Raloxifene [Evista]
Func. class: Bone resorption inhibitor
Chem. class: hormone modifier, SERM
Actions: tissue-selective estrogen agonist/antagonist, agonist activity in bone and on lipid metabolism,
antagonist activity on breast and uterus; reduces reabsorption of bone and decreases turnover rate. Falling
estrogen levels  increases osteoclasts  increases bone reabsorption.
Uses: Reduces overall fracture risk by 24%.
Side/Adverse Effects: none listed
Teriparatide [Forteo]
Func. class: Parathyroid hormone (rDNA)
Chem. class: Teriparatide
Actions: contains human recombinant parathyroid hormone to simulate new bone growth. Only
osteoporosis drug that increases bone deposition (others decrease bone reabsorption). Activates both
osteoclasts (bone reabsorption) and osteoblasts (deposition), but latter predominates. Increases bone
mineral density 2x biophosphates
Uses: osteoporosis, hypoparathyroidism
Side/Adverse Effects: osteosarcoma – serious SE!
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5
RESPIRATORY AND GASTROINTESTINAL DRUGS
Drugs for Asthma
Salbutamol/albuterol [ventolin]
Fun. Class: Adrenergic B2-agonist, sympathomimetic, bronchodilator
Actions: 1st line drug. Inhaled only. NOT anti-inflammatory Causes bronchodilation by action on B2
(pulmonary) receptors. SABAs (short-acting), begin immediately / peak 30-60 min / lasts 3-5 hours. Abort
ongoing attack – generally not for prophylaxis.
Uses: prevention of exercise induced asthma, acute bronchospasms, bronchitis, emphysema,
bronchiectasis, or other reversible airway obstruction.
Side/Adverse Effects: OD increased HR, angina, cardiac arrest, seizure, death.
Ipratropium [Atrovent, others]
Fun. Class: Anticholinergic, bronchodilator
Chem. Class: Synthetic quaternary ammonium compound
Actions: inhibits interaction of Ach at receptor sites on the bronchial smooth muscle  decreases
bronchospasm. Mechanism different than B2 agonists, so use together. Inhalation agent.
Uses: long-term/PRN relief of COPD. Used off label for asthma, but PRN only.
Side/Adverse Effects:
Salmeterol [Advair, others]
Fun. Class: B2-Adrenergic agonist (long acting), bronchodilator.
Actions: 1st line drug. Inhaled or PO. NOT anti-inflammatory Causes bronchodilation by action on B2
(pulmonary) receptors. Abort ongoing attack – but all for prophylaxis – not PRN. Combined with
glucocorticoid.
Uses: prevention of exercise induced bronchospasm, COPD, asthma.
Side/Adverse Effects: LABA’s should never be taken without a glucocorticoid because they may mask airway
inflammation, and an acute exacerbation could be fatal.
Theophylline [Slo-Bid, others]
Fun. Class: Bronchodilator, spasmolytic
Chem. Class: methylxanthine
Actions: Exact mechanism unknown, relaxes smooth muscle of respiratory system by blocking
phosphodiesterase. CNS/cardiac stimulants, vasodilators, diuretics. Administered PO/IV – not active when
inhaled.
Uses: bronchial asthma, bronchospasm associated with chronic bronchitis, emphysema.
Side/Adverse Effects: Periodic measurement of theophylline blood levels essential (< 111umol/L =
therapeutic; 111-140 = N/V, diarrhea, insomnia, restlessness; >167 = severe dysrhythmias, Rx resistant,
convulsions, cardiorespiratory collapse, death). Replaced by safer/more effective Rx.
6
Drugs for Peptic Ulcer Disease
Cimetidine [Tagamet, others]
Fun. Class: H2-histamine receptor antagonist
Chem. Class: Imidazole derivative
Actions: Inhibits histamine at H2-receptor site in the gastric parietal cells, which inhibits gastric acid
secretion. First choice drug for gastric/duodenal ulcers.
Uses: Gastric/duodenal ulcers (short term/acute treatment/prophylaxis), GERD, Zollinger-Ellison Syndrome,
prevention of aspiration pneumonia.
Side/Adverse Effects: none listed
Omeprazole [Losec]
Fun. Class: Antiulcer, proton pump inhibitor
Chem. Class: Benzimidazole
Actions: (most effective for) Supresses gastric acid secretion by inhibiting hydrogen/potassium ATPase
enzyme system in gastric parietal cells. Is a prodrug – converted inside the parietal cells of stomach to
active form.
Uses: Short term Rx (4-8 wk.): duodenal/gastric ulcers, GERD; Long term Rx: hypersecretory conditions
(e.g. Zollinger-Ellison).
Side/Adverse Effects: Short term Rx: H/A, NVD, pneumonia; Long term Rx: Gastric CA, decreased Ca2+
absorption, MI, dementia, kidney disease, early death.
Increased risk for severe diarrhea from C difficile.
Sucralfate [Carafate, Sulcrate]
Fun. Class: Protectant, antiulcer
Chem. Class: Aluminum hydroxide, sulfated sucrose
Actions: Forms a complex that adheres to ulcer site, absorbs pepsin. Creates a protective barrier against
acid/pepsin. Compliments natural mucosal layer. No acid-neutralizing capacity/doesn’t decrease acid
secretion.
Uses: Duodenal ulcer, oral mucositis, stomatitis after radiation of head and neck.
Side/Adverse Effects: May impede absorption of some drugs.
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Other Gastrointestinal Drugs
Aprepitant [Emend]
Fun. Class: antiemetic
Chem. Class: miscellaneous
Actions: Selective antagonist of human substance P/neurokinin 1 (NK1) receptors that decreases emetic
reflex. Fosaprepitant is the prodrug  aprepitant.
Uses: Prevent postop N/V and CINV (Chemotherapy induced N/V).
Side/Adverse Effects: none listed.
Nabilone [Cesamet]
Chem. Class: Cannabinoids
Actions: Nabilone structural analogue of S9-THC (main psychoactive agent in marijuana). Activate
cannabinoid receptors in vomiting centre.
Uses: For CIN/V, also stimulate appetite in AIDS patients.
Side/Adverse Effects: temporal disintegration/dissociation/dysphoria. Contraindicated in patients with
psychiatric disorders.
Infliximab [Remicade, others]
Fun. Class: biologic response modifiers
Chem. Class: tumor necrosis factor modifiers
Actions: Immunomodulator  monoclonal antibody that neutralizes the activity of tumor necrosis factor
alpha found in Crohn’s disease; decreased infiltration of inflammatory cells. Were 2 nd line, now used early
to induce/maintain remission.
Uses: Crohn’s disease, IBD.
Side/Adverse Effects: infections, thrombocytopenia/leukopenia, HF, anaphylaxis.
Mercaptopurine [Purinethol]
Fun. Class: Antineoplastic-antimetabolite
Chem. Class: Purine analog
Actions: Immunosuppressant Inhibits purine metabolism at multiple sites, which inhibits DNA and RNA
synthesis. Azathioprine  mercaptopurine in body. Onset of effects delayed up to 6 months. More toxic
than aminosalicylates/glucocorticoids. Promotes short term remission with Crohn’s.
Uses: IBD, Crohn’s,
Side/Adverse Effects: none listed
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Ondansetron [Zofran]
Fun. Class: antiemetic
Chem. Class: 5-HT3 antagonist (serotonin receptor antagonist)
Actions: Prevents N/V by blocking serotonin peripherally, centrally, and in the small intestine. Most
effective drug for chemo/radiation therapy, anesthesia. Doesn’t block DA receptors= no EPS (akathisia,
acute dystonia).
Uses: Prevention of N/V associated with Cancer chemotherapy.
Side/Adverse Effects: none listed
Sulfasalazine [Salazopyrin, SAS]
Fun. Class: GI anti-inflammatory, antirheumatic
Chem. Class: sulfonamide
Actions: prodrug to deliver sulfapyridine and 5-aminosalicylic acid to colon; anti-inflammatory in connective
tissue also. Antibiotic not used for infection. Metabolized by intestinal bacteria.
Uses: mild-moderate IBD and maintain remission.
Side/Adverse Effects: none listed.
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CANCER DRUGS
Cancer Chemotherapy Drugs: Cytotoxic Agents
Cyclophosphamide [Procytox]
Func. class: Atineoplastic alkylating agent
Chem. class: nitrogen mustard
Actions: Alkylates DNA, is responsible for cross linking DNA strands; activity is not cell-cycle-phase specific
Uses:
Side/Adverse Effects:
Doxorubicin [Caelyx]
Func. class: Antineoplastic, antibiotic
Chem. class: Anthracycline glycoside
Actions: Cytotoxic; Inhibits DNA synthesis primarly; replication is decreased by binding to DNA, which
causes strand splitting; active throughout entire cell cycle. Flat-intercalates DNA (disorts structure/function)
Uses:
Side/Adverse Effects: dysrhythmias within min: usually last < 2 weeks, severe bone marrow depression,
delayed, Rx-resistant cardiotoxicity can develop mo-yr later. Cumulative life dose < 550mg/m^2.
Methotrexate [Metoject]
Func. class: Antineoplastic antimetabolite (vesicant)
Chem. class: Folic acid antagonist
Actions: Inhibits an enzyme that reduces folic acid, which is needed for nucleic acid synthesis in all cells;
Inhibits DNA/RNA/Protein biosynthesis; specific to S phase of cell cycle; immunosuppressive. Inhibits
dihydrofolate reductase  apoptosis. Leucovorin rescue allows massive doses of methotrexate (but failure
to administer leucovorin with 24-48 can be fatal).
Uses:
Side/Adverse Effects:
Cancer Chemotherapy Drugs: Hormonal Agents, Biological Response Modifiers, and Targeted
Drugs
Anastrozole [Arimidex]
Func. class: Antineoplastic
Chem. class: Aromatase Inhibitor
Actions: Highly selective nonsteroidal aromatase inhibitor that lowers serum estradiol concentrations; many
breast cancers have strong estrogen receptors. Do not block production of E by ovaries. No role with
PREmenopausal female (may increase estrogen).
Uses: Advanced breast cancer carcinoma in estrogen-receptor-positive patients (postmenopausal).
Side/Adverse Effects: No endometrial cancer risk, clots rare but increased fracture risk and myalgias.
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Bevacizumab [Avastin, Mvasi, Zirabev]
Func. class: Antineoplastic
Chem. class: monoclonal antibody  angiogenesis inhibitors (blood vessels)
Actions: Supress formation of new blood vessels: solid tumors have no blood supply needed for continued
growth. Monoclonal antibody selectively binds to and inhibits activity of human vascular endothelial growth
factos (VEGF) to reduce microvascular growth and metastatic disease progression.
Uses: colon/lung CA
Side/Adverse Effects: GI perforation, hemorrhage, and thromboembolism.
Imatinib [Gleevec]
Func. class: Antioplastic
Chem. class: Protien-tyrosine kinase inhibitor
Actions: Inhibits Bcr-Abl tyrosine kinase created in patients with chronic myeloid leukemia (CML). Also
inhibits tyrosine kinase.
Uses: Refractory colorectal CA, carcinoma of head/neck
Side/Adverse Effects:
Rituximab [Rituxan, Truxima]
Func. class: Antineoplastic, DMARDs
Chem. class: Murine/human monoclonal antibody; CD20-Directed Monoclonal antibodies
Actions: used to Rx B-cell tumors (e.g. Non-Hodgkin’s lymphoma). CD20 found uniquely on immune system
B-cells. So antibodies ‘only’ injure malignant (and normal) B lymphocytes.
Uses:
Side/Adverse Effects:
Trastuzumab [Herceptin, Kadcyla, Kanjinti, Ogivri]
Func. class: Antineoplastic
Chem. class: Humanized monoclonal antibody
Actions: DNA derived monoclonal antibody selectively binds to extracellular portion of human epidermal
growth factor receptor 2 (HER2); it inhibits the proliferation of cancer cells. Transmembrane receptor that
helps regulate cell growth. Inhibits cell proliferation. Promotes Ab-dependant cell death.
Uses: Breast cancer metastatic with overexpression of HER2, early breast cancer.
Side/Adverse Effects: Cardiotoxicity/potentially fatal hypersensitivity rxns.
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INFECTIOUS DISEASES
Drugs that Weaken the Bacterial Cell Wall I.
Ampicillin [---]
Fun. Class: anti-infective – broad spectrum
Chem class: Aminopenicillin
Actions:
Uses:
Side/Adverse Effects: Most common drug allergy. Can start as a minor rash and next exposure can cause
full blown anaphylaxis. Prior exposure can be without prior treatment (eat fungi/foods of animal origin).
Allergic to one PCN = allergic to all PCNs. Rx. With epinephrine and respiratory support.
Penicillin G [Bicillin]
Fun. Class: Broad spectrum – anti-infective
Chem class: Natural Penicillin
Actions:
Uses:
Side/Adverse Effects: Most common drug allergy. Can start as a minor rash and next exposure can cause
full blown anaphylaxis. Prior exposure can be without prior treatment (eat fungi/foods of animal origin).
Allergic to one PCN = allergic to all PCNs. Rx. With epinephrine and respiratory support.
Drugs that Weaken the Bacterial Cell Wall II.
Cephalexin [Cephalex, etc]
Fun. Class: anti-infective
Chem class: Cephalosporins – 1st Generation
Actions: Beta-lactam antibiotics similar to PCNs. Also weaken the bacterial cell wall and deactivated by
bacteria using beta-lactamases. Inhibits bacterial cell wall synthesis, renders cell wall osmotically unstable.
Uses: Most widely used group of antibiotics. 1st generations only for infections caused by sensitive
staphylococci.
Side/Adverse Effects: Allergic reactions are most frequent adverse rxn. Severe/immediate rxns are rare. 1%
of pts: cross-reactivity between cephalosporrins to pts with h/o severe PCN reactions.
Vancomycin [Vancocin]
Fun. Class: Anti-infective
Chem class: Tricyclic glycopeptide
Actions: Does not interact with PCBs – targets precursor molecules for cell wall biosynthesis.
Uses: Most widely used antibiotic used in U.S hospitals. Mainly for: CDI, MRSA, Rx serious infections with
susceptible organisms in patients allergic to penicillin.
Side/Adverse Effects: Dose related renal failure, hearing impairment: rare, reversible. Monitor blood
levels!
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Bacteriostatic Inhibitors of Protein Synthesis
Erythromycin [Benzamycin, Eryc, Erythro, Erythrocin]
Fun. Class: Anti-infective
Chem class: Macrolide
Actions: Mechanism/bacterial resistances similar to tetracyclines – but bind to 50s ribosomal unit.
Uses:
Side/Adverse Effects: one of our safest antibiotics.
Tetracycline [Tetra]
Fun. Class: Broad spectrum – anti-infective
Chem class: Tetracycline
Actions:
Uses:
Side/Adverse Effects: stains teeth, superinfection (overgrowth of 2nd bug) because broad spectrum.
Produces C difficile – life threatening diarrhea.
Aminoglycosides
Streptomycin [--]
Chem class: Aminoglycoside
Actions: Bactericidal inhibitor of protein synthesis – rapid bacterial cell death.
Uses: used against aerobic gram negative bacilli. Would have been effective against the black plague.
Side/Adverse Effects: Monitor serum drug levels! Ototoxicity: accumulates within inner ear, can impair
hearing and balance. Ear ringing, high frequency loss, H/A – nausea/dizziness/vertigo. Nephrotoxicity:
proteinuria, dilute urine, increased creatinine. Aminoglycosides themselves accumulate – more damage to
kidney and ear. Injury reverses following drug cessation. Inhibit neurotransmission: flaccid paralysis and
potentially fatal respiratory depression.
Sulfonamides and Trimethoprim
Trimethoprim-Sulfamethoxazole [Sulfatrim, Trimel]
Fun. Class: Anti-infective
Chem class: Sulfonamide
Actions: Act together to inhibit sequential steps in folic acid synthesis. Resistance less than either drug
alone.
Uses: UTIs. Rx choice of pneumocystis pneumonia (PCP) in HIV/AIDS.
Side/Adverse Effects:
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Antiviral Agents I.
Acyclovir [--]
Fun. Class: Antiviral
Chem class: Purine nucleoside analog
Actions: Inhibits viral replication by supressing synthesis of viral DNA. Selectivity: virus activates drug.
Resistance: virus has mechanisms that interfere with activation.
Uses: Agent of 1st choice for HSV/VZV. HSV genitalis;
HSV mucocutaneous (face/oropharynx)  oral: primary for infections, prevent recurrences
(immunocompetent). IV: immunocompromised patients (severe infection).
Varcilla-Zoster: Oral: for herpes zoster (shingles), also for varicella (chickenpox) in children and
adults. IV: immunocompromised patients.
Side/Adverse Effects: Serious SEs uncommon.
Influenza vaccine [FluMist, Influvac, others]
Actions: 3 Basic kinds: Inactivated (IV); Recombinant hemagglutinin (RIV); Live attenuated (LAIV). Changed
yearly based on WHO/FDA/CDC prediction. Oct/Nov best vaccination time. Protection begins 1-2 weeks
after administration and lasts more than 6 months.
Uses: Influenza A (96%)/B
Side/Adverse Effects: Significant SEs very rare. Small risk of Guillain-Barre: paralysis, including respiratory
muscles.
Lamivudine [--]
Fun. Class: Antiviral
Chem class: Nucleoside reverse transcriptase inhibitor (NRTI).
Actions: Inhibits replication of HIV virus by incorporating into cellular DNA by viral reverse transcriptase,
thereby terminating cellular DNA chain.
Uses: Hepatitis B. also active against HIV.
Side/Adverse Effects: May promote emergence of resistant HIV if co-infected. Relapse after treatment is
stopped. Rx prolonged: increased adverse effects/costs.
Oseltamivir []
Fun. Class: Antiviral
Chem class: Neuraminidase inhibitor
Actions: Inhibits influenza virus neuraminidase with possible alteration of virus particle aggregation and
release.
Uses: Current drug of choice for influenza A/B, swine flu. Given PO.
Side/Adverse Effects:
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Antiviral Agents II.
Darunavir [Prezista]
Fun. Class: Antiretroviral
Chem class: Protease inhibitor [step 10]
Actions: Among the most effective (combo with NTRIs).
Uses: HIV-1
Side/Adverse Effects: fat maldistributed, diabetes, decreased bone density, increased bleeding, increased
triglycerides.
Enfuvirtide [Fuzeon]
Fun. Class: Antiviral (new)
Chem class: Fusion inhibitor [step 2]
Actions: HIV fusion inhibitor – inhibitor of the fusion of HIV-1 with CD4+ cells.
Uses: HIV-1. 2x/day shots + $20K/yr
Maraviroc [Celsentri]
Fun. Class: Antiretroviral
Chem class: Fusion Inhibitor, CCR5- receptor antagonist [step 1]
Actions: interfears with entry into HIV-1 by inhibiting the fusion of the virus and the cell membrane.
Uses: HIV-1
Raltegravir [Isentress]
Fun. Class: Antiretroviral
Chem class: HIV integrase strand transfer inhibitory (ISTIs) [Step 5]
Actions: inhibits catalytic activity of HIV integrase, which is an HIV-encoded enzyme needed for replication.
Uses: HIV
Zidovudine [AZT, Retrovir]
Fun. Class: Antiretroviral
Chem class: Nucleoside reverse transcriptase inhibitor (NRTI)  [step 3]
Actions: Inhibits replication of HIV-1 virus by incorporating into cellular DNA by viral reverse transcriptase,
thereby terminating the cellular DNA chain. Incorporates into growing DNA, foil reverse transcriptase 
step 3.
Uses: HIV-1
Side/Adverse Effects: High doses lead to low RBCs/WBCs. Rare: lactic acidosis/hepatomegaly.