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Mechanism of Action Competitive inhibitor of nucleic acid polymerases (when inserted instead of base missing hydroxyl group so no phosphodiester bond suicide substrate, chain terminator)


Adverse Effects Generally well tolerated but high IV dosing can cause nephrotoxicity and neurotoxicity Drug resistance acan dveleop with mutation in viral TK or viral DNA pol Can have as much as 50% in CSF Can interact with AZT(severe lethargy) and nephrotoxic drugs transient mild moderate GI distress, minimized with food eliminated primarily unchanged in the kidneys so decrease dose in kids and those with renal impairment


Influenza A and B, treat within Selective Neuraminidase 48 hrs of onset, reduces time of inhibitor; sialic acid analogues, illness inhibit viral neuraminidase, which cleaves sialic acid residues to facilitate release from host cell (stop viral release from cell)

Zidovudine (AZT)

Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTI) Fully phosphorylated forms (i) compete for RT, and (ii) function as chain terminators block viral replication

suppression of HIV infection; elevate CD4 counts, AZT use during pregnancy reduces HIV transmission to fetus

Indinavir (IDV)

inhibition of HIV protease, which HIV, combination therapy essential for the production of mature, mediates posttranslational processing of viral gene products, cleaves itself then other products

- metabolized primarily via cytochrome CYP3A4, other drugs acted on CYP3A4 may accumulate to dangerous levels other drugs inducing CYP3A4 may increase metabolism - resistance develops rapidly, buffalo hump, due to fat redistribution also hyperglycemia, nephrolithiasis - absorption of this drug impaired by high fat meal Generally well tolerated but 10% have allergy to whole class GI problems: nausea, diarrhea vomiting penicillins work best against actively growing bacteria, thus bacteriostatic antibiotics (chloramphenicol, macrolides, tetracyclines) interfere with their activity low pH, dextrose solns, aminoglycosides solns:

Penicillin G

lactam ring fused to five membered thiazolidine ring and R group; lactams irreversibly inhibit transpeptidases and decrease cross-linkage of glycan strands compromising the cell wall less susceptible to lactamase

Bactericidal at therapeutic concentrations

inactivate lactam probenecid (gout) blocks renal excretion, active lactam in blood longer Superinfection with Clsotridium difficile; alteration of normal flora allows this bacteria to grow; produces toxin causing diarrhea GI: diarrhea, nausea, vomiting most common with this combination drug Prolonged use causes biliary sludging (pain, nausea, vomiting) in up to 43% metals chelate quinolones, block adsorption; many antacids, some dietary supplements; take quinolones 2 hrs prior or 2-6 hrs after digesting metals Avoid in children, pregnant/nursing women (damage growing cartilage) avoid in patients taking drugs prolonging QT


Inhibit cell wall synthesis

Amoxicilin/Clavulanic Acid (Augmentin) Ceftriaxone Ciprofloxacin

Amoxicillin Inhibit cell wall synthesis and clavulanic acid is a lactamase inhibitor Cephalosporin; inihibit cell wall synthesis are bactericidal and target topoisomerases which increased the supercoiling of DNA which impacts DNA replication, repair and transcription tolerated by humans well because the drug has a greater affinity for bacterial topoisomerases and bacteria are actively growing (replicating and repairing DNA more)

broader spectrum activity 3rd generation, broader spectrum activity



Recurrent UTIs, opportunistic infections in AIDS

interval, arrhythmias, fainting antifolate activity in humans, may be offset with supplement folic acid; nephrotoxicity avoid in renal impaired Contraindication: hepatic impairment Antacids lower the serum level of Azithromycin GI: cramps, diarrhea, nausea, vomiting Contraindication: hepatic impairment Drug Interactions: Erythromycin inhibits the cytochrome P450 System (CYP3A4); interactions common with other drugs metabolized by CYP3A4 stimulates GI motility; GI intolerance may force switch of drug


Protein synthesis inhibitors; bacteriostatic

treat infections caused by Gram-positive bacteria; also works well against several Gram-negatives


Protein synthesis inhibitors; bacteriostatic

treat infections caused by Gram-positive bacteria


Protein synthesis inhibitors; bacteriostatic

Cardiotoxicity: arrhythmia, do not administer wih drugs that prolong QT interval Caution: children under 8 years; pregnant lactating (category D); patients with liver impairment GI distress in some cases GERD, Photosensitivity Skeletal: avoid use in children as drug binds bones and teeth


inhibits DNA-dependent RNA polymerase, blocks txn binds to bacterial form with greater affinity than eukaryotic counterpart

combo treatments (TB, leprosy); Also inhibits many G+ and G- bacteria; Prophylaxis of meningococcal and H. influenzae meningitis

generally well-tolerated, minor hepatotoxicity, usually in patients with prior liver problems induces P450 enzymes; increases metabolism of drugs processed by P450 enzymes hepatotoxicity, peripheral neuritis can offset with pyridoxine (vit B6), rash, convulsions in patients prone to seizure


inhibits mycolic acid (FA) synthesis, a unique component of mycobacterial cell walls

Used alone for prophylaxis, in combo to treat TB Bactericidal for growing forms Bacteriostatic for resting forms

Amphotericin B

binds ergosterol and forms pores most systemic fungal infections, on the membrane some protozoa

amphoterrible, fever and chill (shake and bake), hypotension, nausea, nephrotoxicity(80%) caution with other nephrotoxic drugs, arrhythmias caution in use: renal impairment


interfere with ergosterol synthesis (inhibit SQUALENE EPOXIDASE) accumulate toxic squalene compromise integrity of membrane interfere with ergosterol synthesis, inhibits Lanosterol 14- Demetylase, a cytochrome P450 enzyme binds microtubules- mitosis inhibitor (causes multinucleated cells)

dermatophytes nail fungus (onychomycosis), jock itch (T. cruris), athletes foot (T. pedis)

generally well tolerated, avoid if pregnant/nursing or if liver/kidneys impaired


Broad spectrum

avoid azoles in pregnancy


restricted to dermatophyes (skin, hair and nail infections), alternate treatment for onychomycosis (nail), ringworm caused by Microsporum, Epidermophyton

Generally well tolerated; headaches other CNS effects, photosensitivity and rash

or Trichophyon TMP/SMX Metronidazole ETS generates damaging free radical when metabolizing Metroidazole Pneumocystis juroveci pneumonia (PCP) anaerobic protozoa and bacteria, e.g. Helicobacter, Clostridium rash, hepatitis,; neutropenia, azotemia, thrombocytopenia usually mild; headache, nausea, dry mouth, metal taste, GI distress, disulfiram effects avoid alcohol Chloroquine radiolabeled chloroquine binds to toxic heme in the parasite food vacuole drug bound heme cannot polymerize; parasite dies in its own waste (oxidative damage) Quinine/ Quinidine Gluconate inhibition of heme polymerization effective against erythrocytic foms of Plasmodium effective against erythrocytic forms of Plasmodium, used for prophylaxis and treatment generally safe for children generally well tolerated, safest quinolone Contraindications: not recommended for pateints with epilepsy or MG, do not give to patients with psoriasis more toxic, less effective use in combo therapy Contraindications: not recommended for patients with epilepsy and MG metabolized extensively by hepatic P450 system

Sulfadiazine + Pyrimethamine Mebendazole

DHPS & DHFR inhibitor, resp.; blocks production of THFA Inhibits microtubule polymerization/mitotic spindle poison; bind worm -tubulin with higher affinity than mammalian orthologue kills larvae in host not effective against adult worm; induces paralysis via glutamate gated Clchannels found only in invertebrates causes spastic paralysis and tegument damage

Toxoplasma, antimalarial, antibacterial nematodes/roundworms

allergies to sulfa, pyrimethamine toxicity (bone marrow suppression), does not alleviate encysted form Generally well tolerated


broad spectrum antiparasitic; nematode, esp. for filariae causing onchocerciasis (river blindness) flatworms and cestodes

Can effect mammalian GABA receptor so contraindicate when Blood Brain Barrier is impaired generally well tolerated, GI distress, CNS effects Contraindications: ocular cysticercosis (tapeworm larvae in eye) as host response to dead worm damages eye; ophthalmologic surgery is recommended instead inducers of CYP reduce bioavailability of drug Hypoglycemia;



Type 1 DM; IDDM

impaired neurologic function. inability to concentrate. slurred speech, lack of coordination, staggering symptoms are often mistaken as alcohol intoxication Glipizide increasing endogenous insulin secretion; ATP binds to KIR and blocks the channel ADP binds to SUR and activates the channel SUR enhances sensitivity of KIR to ATP and interacts with sulfonylureas and meglitinides increasing endogenous insulin secretion ; ATP binds to KIR and blocks the channel ADP binds to SUR and activates the channel SUR enhances sensitivity of KIR to ATP and interacts with sulfonylureas and meglitinides Decrease ATP sensitive K+ Type 2, NIDDM hypoglycemia Oxidized to inactive metabolites Half-life - 2 to 4 hours Potency - High (2.5 to 40 mg/day)


Type 2, NIDDM Oxidized to weakly active metabolites Half-life - 6 hours Duration of action - 24 hours Potency - High (1.25 to 20 mg/day) Tyoe 2, NIDDM



Effect is rapid and brief so


channel conductance Act similarly too sulfonylureas but bind to distinctly different region of SUR1 Insulin sensitizers; antihyperglycemics; Correct elevated hepatic glucose output Inhibit hepatic gluconeogenesis Inhibit glucose-6-phosphatase activity inhibit glycogenolysis activity of insulin receptors insulin resistance are agonists of -(PPAR) activation of PPAR alters the rate of expression of a number of genes encoding proteins involved in regulating lipid and glucose metabolism, ultimately increasing sensitivity to insulin at the target tissues competitive and reversible inhibitors of a-glucosidase in the small intestine Delay carbohydrate digestion and absorption Smaller rise in postprandial glucose

reduced risk of long-lasting hypoglycemia Appropriate for obese type 2 diabetics Doesnt produce lactic acidosis or hypoglycemia; Secondarily Reduced triglycerides, total cholesterol, LDL Increased HDL Weight loss, some reduction of blood pressure Reduce hepatic glucose output Does not increase insulin secretion Does not induce weight gain For mild to moderate fasting hyperglycemia with significant postprandial hyperglycemia Gastrointestinal disturbances Flatulence Nausea Diarrhea Contraindicated for inflammatory and obstructive bowel disease, colonic ulcers





opens the KATP channel and inhibits insulin release Synthetic T4 hormone compete with thyroglobulin for oxidized iodide in the process of organification and coupling inhibits T4/T3 conversion compete with thyroglobulin for oxidized iodide in the process of organification and coupling results in selective destruction of thyroid gland high levels of iodide inhibit thyroid hormone synthesis and release (Wolff-Chaikoff effect) inhibit peripheral T4/T3 conversion by 5-deiodinase inhibit mevalonate pathway in

Oral agent for hypoglycemia of various causes, including insulinomas Hypothyroidism Hyperthyroidism Propylthiouracil inhibits both thyroid peroxidase and T4/T3 conversion Hyperthyroidism methimazole inhibits only thyroid peroxidase; more potent than propylthiouracil hypothyroidism Hyperthyroidism used to block thyroid function in radiation emergencies Hyperthyroidism Inihibit peripheral thyroid metabolism Pagets disease and hypothyroidism Rare but excessive dose produce symptoms of hyperthyroidism

Levothyroxine Propylthiouracil


Radioactive iodide Stable Iodide



not to be used in the presence

osteoclasts, posttranslational modification slow or block bone resorption, thus, help to lower serum calcium levels

postmenopausal osteoporosis in women

of hypocalcemia, during pregnancy or lactation, or with a history of any allergy to bisphosphonates should not be given to anyone who is unable to remain upright for 30 min after taking the drug, then to have a meal serious esophageal erosion can occur! salmon calcitonin should not be used with known allergies to salmon or fish products caution should be used in patients with renal dysfunction could be exacerbated flushing of the face and hands, skin rash, nausea and vomiting, urinary frequency, local inflammation at the site of injection should not be used in the presence of any known allergy to vitamin D, hypercalcemia, vitamin D


binds directly to receptors on osteoclasts and inhibits bone resorption;


Calcitrol Increases absorption of dietary calcium in small intestines Vit D compound reatment of hypoparathyroidism and in patients undergoing chronic renal dialysis

mineral resorption in bone, and re-absorption of calcium and phosphate from renal tubules inhibit PTH synthesis and release with PTH and calcitonin regulate calcium homeostasis Calcium gluconate a therapy for hypocalcemic states associated with disorders such as vitamin D-dependent rickets and hypoparathyroidism once-daily subcutaneous administration of PTH favors bone anabolism

toxicity metallic taste, nausea, vomiting, dry mouth, constipation, and anorexia CNS effects: weakness, headache, somnolence, irritability less venous irritation than calcium chloride

Parathyroid Hormone

increase in bone formation occurs because PTH acutely promotes osteoblast development and stimulates osteoblast activity stimulates production of active vitamin D in the kidney

cannot be taken orally, only subcutaneously or IV


Inhibition of dihydrofolate reductase (DHFR) which leads to depletion of cofactors required for synthesis of thymidylate and purines

ALL in children, choriocarcinoma, combo therapy for breast carcinomas, head and neck, ovary and bladder high dose used for adjuvant therapy Also for psoriasis, rheumatoid arthritis, immunosuppressive agent

With standard dose myelosuppression, stomatitis, enteritis High dose have conjunctivitis, renal failure neurotoxicity and rarely hepatic failure


Function as analog of natural purine and inhibit de novo purine synthesis and become incorporated into nucleic acids

Myelosuppression, gi and hepatic toxicity


Inhibition of thymidylate synthase, reduced production of TTP increase incorporation of dUTP into DNA

Potent radiosensitizer Intense dense and combo with leucovorin associated with significant gi toxicity, myelosuppression Skin pigmentation and rashes are common Rarely cerebellar toxicity


Inhibition of ribonucleotide reductase; inhibit incorporation of dCTP into DNA by DNA pol

IV administration only

Same toxicities as the class and elevation in liver transaminases Potent radiosensitizer, not to be used with radiotherapy Neutropenia; gi side effects


Bind to tubulin at site that overlaps with GTP binding domain and prevents extension of MTs; chromsomes dont segregate during mitosis

Lymphomas and second line therapy for various solid tumors


Bind to beta tubulin at site distinct from vincas or colchine; promote polymerization and prevent depolymerization arresting cell in mitosis

Treatment of many solid tumors breats, ovarian and lung

Peripheral neuropathy, myalgias, myelosupression Acute hypersensitivity rxns occur possibly die to vector


Same as above, arrests cell in mitosis Same as above, arrests cell in mitosis

Improves survival in men with metastatic prostate cancer by 2.4 months Improves survival in men with metastatic prostate cancer by 4.3 months

Peripheral neuropathy, myalgias, myelosupression Peripheral neuropathy, myalgias, myelosupression



Bind MTs at interface btw alpha and beta tubulins, and destabilize

First used as antiinflammatory/immune Used in association with allopurinol for gout

Immune deficiency, diarrhea


Alkalating agent; alkylates DNA twice inducing crosslinks in the DNA

Metabolite acrolein, can cause severe cystitis, fancoli like syndrome in kidneys CNS: confusion, drowsiness, hallucinations


Standard of care for glioblastomas; lipid soluble can diffuse across BBB Binds DNA repair and potentiates effects of other chemotherapy agenst that damage DNA Intercalate into GC rich regions of DNA, depress DNA,RNA and protein synthesis May metabolize and form free radicals Activate apoptosis signaling pathway


TMZ+ O6- Benzyl Gaunadine


Myelosuppression, alopecia, GI disturbances, cardiac toxicity is marked



Functional groups replaced by water which is replaced by DNA base usually G and crosslinking occurs Functional groups replaced by water which is replaced by DNA base usually G and crosslinking occurs Cause DNA strand breaks by trapping and stabilizing top II Blocks estrogen receptor Blocks GnRH Philadelphia chromosome Interferes with HER2/neu receptor Breast cancer Breast cancer CML Breast cancer

Nephrotoxicity common, highly emetogenic, marked peripheral neuropathy, anemia Nephrotoxicity only in high doses, mildly emetogenic, rarely have peripheral neuropathy, myelosuppression


Tamoxifen Degaralix Imatinib Trastuzumab


IL-6 receptor antagonist (cytokine involved in the development of immunological and inflammatory reactions) antibody that blocks vascular endothelial growth factor A (VEGF-A) which prevents the establishment of blood supply and metastatic spread. RCC, lung cancer, colon cancer to slow growth and inhibit spread


Clomiphene Menotropins/ Urofillitropin hCG

Anti-estrogen , blocks estrogen inhibition of FSH and LH release Produces follicular stimulation Mimics LH,

Used to treat ovarian failure

Possibility for overstimulation multiple pregnancies


Synthetic androgen used to inhibit the output of FSH/LH, removing hormonal stimulation Stimuates the release of LH/FSH Endogenous Major endogenous estrogen in humans Equillan Premarin Slower; orally available Orally effective prodrug; quickly demethylated to ethinyl estradiol

After priming with menotropins for 14 days give hCG to induce follicle ovulation Treatment for endometriosis Any sex steroid can inhibit FSH/LH in either sex

Facial hair, lose hair, and slight virilization

GnRH estradiol Estrone Conjugated estrogens Ethinyl estradiol Mestranol

Must administer in a pulsatile pattern First pass effect so not effective orally Purified mixtures of conjugated steroids with estrogenic properties

Progesterone medroxyprogesterone

Progesterone analogs Progesterone analogs

Progestational activity Progestational activity Slow release form f injected progesterone, once injected slowly ansorbed into circulation, once n circulation they are rapidly transformed and cleared aaw

Norethindrone Drosperinone

Norgesetrel, levonogestrel Mifepristone

Progestational and androgenic activity Anti-androgemic activity and anti mineralcorticoid activity, available in combo type oral contraceptives Progestational and androgenic activity RU- 486 abortion pill