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191 Cards in this Set
- Front
- Back
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Pharmacodynamics
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What drug does to body
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Pharmacokinetics
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What body does to drug
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Phase I of biotransformation
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Drug converts to a more polar metabolite
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Phase II of biotransformation
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Endogenous molecule combines to Phase I metabolite
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Weak acids are removed through
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Active tubular secretion at the proximal tubule
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Dinoprost, dinoprostone and carboprost are
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Prostaglandin drugs used for abortion
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Misoprostol is used in px chronically taking NSAIDs
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To treat gastric ulcer
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Captopril, enalapril and lisinopril are
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ACE inhibitors that help decrease Angiotensin levels
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Saralasin is a drug that
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Blocks Angiotensin receptors
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Kinin drugs (bradykinin and kallidin) are
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The most potent vasodilators – act on arteriole beds
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Serotonin acts on most arteries and veins causing
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Constriction – dilates skeletal m vessels
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Tryptophan helps to
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Increase rate of serotonin synthesis (an indolamine)
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Tricyclic antidepressants (imipramine) inhibit the
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Receptor mediated uptake of serotonin by neurons
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MAO inhibitors inhibit the
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Degradation of serotonin
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Reserpine and tetrabenazine act to
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Deplete neuronal stores of serotonin – cause depression
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Ergot alkaloids like ergotamine, methysergide and bromocriptine are used to treat
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Migraines and postpartum hemorrhaging
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Tx of asthmaAdrenergic agonists B2 selective adrenergic agonistsTheophyllineCromolyn sodiumCorticosteroidsAnticholinergic agents
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Epinephrine, ephedrine and isoproterenol (bronchdilation)Metaproterenol, terbutaline and albuterol (bronchodilatin)Bronchodilator – overdose cause seizures and arrhythmiaStabilizes mast cell membrane – block Ca gates Beclomethasone, flunisolide, triamcinolone, methylpredAlternative to adrenergic agonists
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Non systemic antacids for GI upset include
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Calcium carbonate, aluminum and magnesium hydroxide
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Sucralfate acts to
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Bind t necrotic ulcer tissue – barrier to HCl and pepsin
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Colloidal bismuth coat and bind to both
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Gastric and duodenal ulcer tissue – protect from acid/pepsin
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Disinfectant alcohols include
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70% ethanol, 90% isopropanol – do not kill spores
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Disinfectant aldehydes include
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1-10% formaldehyde (kills microbes and spores by protein precipitation) 2% glutatldehyde in 70% isopropanol – for instruments
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5% boric acid is used for
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Skin lesions but is fairly toxic
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0.1 % benzoic acid is used as a
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Food preservative
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Salicylic acid is used as a
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Skin fungicide
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1% acetic acid is used as a disinfectant in
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Surgical dressings
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0.005% iodide is cidal to
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Bacteria and spores
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10% provodone iodide (Betadinem Isodine)
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Skin disinfectant
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Chlorine is used to disinfect water at
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20ppm
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Potassium permanganate is an oxidizing agent used to
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Disinfect weeping skin lesions
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Nafcillin is a
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Narrow spectrum penicillin–NOT susceptible to B lactamase
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Cephalosporins are active against
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G- bacteria, E.coli, Klebsiella
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Bacitracin is only used as a
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Topical ung for G+ bacteria – severely nephrotoxic
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Cycloserine is a drug used against
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TB
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Isoniazid inhibits the synthesis of
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Mycolic acid in mycobacteria cell walls (TB)
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Polymixins are used for
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G- infx – lyse cell walls – neuro- and nephrotoxic
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Erythromycin (macrolides) inhibit
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Protein synthesis (bind 50S subunit) – target G+ organisms
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Aminoglycosides bind the
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30S subunit – used for serious G- infx – gentamycin, tobramycin, amikacin, streptomycin, neomycin
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Tetracyclines block
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TRNA at the 30S subunit
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Chloramphenicol binds to the
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50S subunit – can cause aplastic anemia / Gray Syndrome
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Sulfonamides inhibit
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Nucleic acid synthesis
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Rifampin is used to treat infx with
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Mycobacterium leprae – binds RNA polymerase
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Actinomycin acts by
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Binding DNA to block RNA synthesis
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Polyene drugs work by binding to NystatinAmphotericin BNatamycin
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Ergosterol in fungal membranes – Too toxic for systemic use – used topicallyVery toxic – used for systemic mycosesUsed for most eye fungal infx – low toxicity
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Imidazole drugs (ketoconazole) inhibit the
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Synthesis of ergosterol – less toxic
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Griseofulvin is a drug used to treat
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Dermatophytic infx – bonds tubulin
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Flucytosine is a nucleic acid analog that alters the
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Function of fungal RNA – used only for Crypto and Candida – causes reversible bone marrow inhibition
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Sulfones and sulfonamides are used to treat
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Malaria, toxoplasmosis and coccidiosis
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4 hydroxyquinoline derivatives are used to treat
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Coccidiosis – inhibit mitochondrial respiration
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Benzimidazole derivatives
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Infx with a nematode can be treated with
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-ganglionic nictonic Ach agonist or-GABA agonist (piperazine)
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Praziquantel is used as an
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Antischistosomal and anti tapeworm agent
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Absorption and penetration of a virus is inhibited by
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-amantidine (prevent release)-gamma globulins (prevent entry)-moderate to high pH
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DNA ploymerases are affected by
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Vidaribine, acyclovir and cytarabine
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Amantidine
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Tx influenza A and rubella – block penetration into host cell
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Idoxuridine (IDU) – thymidine analog
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Makes DNA defective – tx HSV keratitis, CMV and vaccinia – topical only due to bone marrow suppression, GI damage, hair loss and hepatotoxicity
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Cytarabine (ara-C)
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Used for IDU resistant HSV keratitis also for anticancer tx
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Trifluorothymidine (trifluridine) –pyrimidine metabolite
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Less toxic than IDU
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Vidarabine – purine analog
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Tx HSV, VZV, - less toxic than IDU
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Acyclovir
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Inhibits viral DNA polymerase – tx HSV I, VZV,EBV – IV use can causehallucinations, seizures, nephrtoxicity
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Azidothymidine (AZT) – reverse transcriptase inhibitor
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Tx HIV – toxic to bone marrow
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Interferons are used to treat
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HBV, Zoster suppression and cancer tx
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Methisazone is usedto tx
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Small pox (variola) , vaccinia
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Rifampin is used
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Topically for vaccinia lesions
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Tamoxifen is an
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Estrogen inhibitor used to prevent metastatic breast CA
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Carmustine (BCNU) alkylating agent used to tx
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Metastatic CA – injected into internal carotid A
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NSAIDsAspirin (Salicylic acid) works byIbuprofen works by
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Irreversible inhibition of cyclooxygenase – anti-inflammatory, analgesic and antipyreticReversible inhibition of cyclooxygenase – may decrease effectivness of aspirin
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To control rheumatoid inflammation can use
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Hydroxychloroquine (malaria med) and gold salts
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Opioid drugs – Morphine, heroin, codeine)
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Aka narcotic analgesics – used to tx severe, constant pain-undergo 1st pass hepatic metabolism – excreted renally
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Opiates effect different receptorsMuKappaSigma
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Analgesia and physical dependenceSpinal analgesiaHallucinations and cardiac stimulation
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Side effects of opiates include
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Sedation, nausea, vomiting, respiratory depression, miosis, bradycardia, euphoria and constipation
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An antagonist of the opiates is
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Naloxone
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Tylenol (acetaminophen) has
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Analgesic effects but no anti inflammatory effects
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Sedative hypnotics are used to tx
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Anxiety, convulsions and sleep disorders
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Ethanol has very steep dose response curve
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Benzodiazepines have a shallow dose response curve – safest of the sedative hypnotics
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Used to treat anxiety – Diazepam (valium), chlordiazepoxide (Librium), alprazolam (Xanax)
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Barbiturates have a steep curve
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Clonidine is a hypertensive drug used to tx
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Panic attacks
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AntipsychoticsTricyclics (phenothiazines)Heterocyclics (butyrophenones)
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Block dopamine receptors – Parkinson-like side effects Chlorpromazine, fluphenazine – fewer side effects
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AntiparkinsonismLevodopaBromocriptinePergolide (Permax)MAO inhibitorsCatecholomethyltransferase (COMT)InhibitorAmantadineAcetylcholine blocking drugs
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Penetrates the BBB and is converted to dopamineAn ergt derivative – acts on dopamine receptorsDirectly stimulates D1 and D2 receptors – prolongs response to levodopaRetards breakdown on dopa – prolongs effect of levodopaCOMT competes with LevodopaAntiviral c antiparkinsonian effects – mechanism unknownAntimuscarinic drugs
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Tricyclic antidepressants
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Imipramine, amitriptyline, doxepinBlock reuptake of norepi – beneficial effects ~3wks
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MAO inhibitors
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Inhibit destruction of norepi in the presynaptic terminal
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Second generation antidepressants
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Tetracyclic drugs (meprotiline)
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Phenytoin (Dilantin) is used to tx
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Partial and grand mal seizures – nystagmus, diplopia, ataxia and sedation
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Phenobarbital is used to tx
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Partial and grand mal seizures
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Primidone
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A barbiturate analog
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Carbamazepine (Tegretol) `
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Blocks reuptake or norepi and blocks Na channel conduction – used in trigeminal neuralgia and partial and grand mal seizures – diplopia dn ataxia
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Benzodiaepines are useful in treating
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Prolonged generalized seizures
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Valproic acid (Depakene) acts on
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GABA to reduce generalized absence seizures
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Four stages of anesthesia1234
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AnalgesiaExcitement – loss of consciousness- enhanced reflexes and irregular respirationSurgical anesthesia – loss of pain reflex, regular respirationMedullary depression – severe respiratory depression requiring ventilation
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All general anesthetics
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Increase the firing threshold of CNS neurons
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Inhaled anesthetics include
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Nitrous oxide, halothane, enflurane, isoflurane
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Thiopental is a short acting
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Barbiturate - induces anesthesia before using inhalants
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Narcotic analgesics in combination with NO are used in
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Px who unable to survive full general anesthesia
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Ketamine is used to produce a
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Dissociative anesthesia – amnesia, analgesia and catatonia
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The prototypical hallucinogenic drug is
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LSD – produces hyperarousal of the CNS
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PCP, angel dust causes a
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Separation of body functions from their minds without causing loss of consciousness
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During anesthesia the order of loss is
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Pain > temperature > touch, proprioception > muscle tone
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Most local anesthetics are
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weakly basic tertiary amines
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Local anestheticsEstersAmides
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Cocaine, proparacaine, tetracaine, benoxinate – metabolized by hydrolysisLidocaine, bupivacaine – metabolized in liver – excreted by kidney
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Anesthetics with a low pKa (high lipid solubility)
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Have faster onset
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GH increases the
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Number of cells – NOT the size of cells
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Thioureylenes (eg. propylthiouracil) act to
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Inhibit the formation of thyroid hormones
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Sulfonylureas are drugs that
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Stimulate the release of insulin from B cells and increase the sensitivity of the tissues to insulin
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Ciglitazone
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Increase the number of insulin receptors
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Glucosidase inhibitors
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Reduce GI absorption of carbohydrates
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Progesterone is mainly secreted by the
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Corpus luteum at the end of the cycle
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The main determinant for the inset of menstruation is
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Progesterone
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The endometrium is maintained during pregnancy by
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Progesterone
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Proliferation of acini of mammary glands is due to
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Estrogen and progesterone
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Thiazide diuretics
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Act on early segments of the distal tubule Bendrofluazide, hydrochlorothiazide, metolazoneMay cause gout. Not used in NIDDM
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Loop diuretics
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Frusemide, bumetanideCan be used in px with impaired renal function – can lead to deafness in high doses
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Potassium sparing diuretics
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Spironolactone (antagonistic to aldosterone )Amiloride and triamcinolone (block Na channels)Act on the aldosterone responsive segments of the distal tubule
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CAI inhibitors
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Depress bicarbonate reabsorption in the proximal tubule Acetazolamide is used to tx glaucoma
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Clonidine (Catapres)
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Stimulates alpha2 receptors to lower BP – used with a diuretic
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Methyldopa (Aldomet)
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Lowers BP – side effects include marked drowsiness, depression and nightmares
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Resperine (Raudixin, Syrosingopine) causes a
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Decrease in catecholamines and serotonin in nerves – causes parasympathetic side effects
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Prazosin (minipress) acts by
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Blocking post synaptic alpha2 receptors on blood vessels – prevents peripheral vasoconstriction – dilates arteries and veins
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Phentolamine
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Blocks alpha 1 and 2 receptors – NOT used in HTN
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Phenoxybenzamine
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Blocks alpha 1 and 2 receptors – NOT used in HTN
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Propranolol blocks
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Beta 1 and 2 – blocks rennin release – reduces CO – used with a diuretic – may induce an asthma attack
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Metoprolol and Atenolol (Tenormin) block
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Only beta 1
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Nadolol (Cogard)
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Guanethidine blocks
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Catecholamine release – does not cross BBB
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Vasodilators Hydralazine (Apresoline)Diazoxide (Hyperstat)Minoxidil (Loniten)Nitroprusside (Nipride)Ca channel blocker (Nifedipine)
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Lower BP by relaxation of vascular smooth muscle Only for emergency – inhibits insulin releaseUsed when nothing else works – cause Na retentionUsed in hypertensive crisis
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Captopril is an
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ACE inhibitor (inhibits angiotensin I to angiotensin II)
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Angiotensin II functions to
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Elevate BP, increase contraction of smooth muscle, mediates release of aldosterone, increase release of catecholamines from adrenal medulla and adrenergic nerves
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Cardiac glycosides (cardenolides) are used to treat Digitalis DigitoxinQuabain
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Congestive heart failure Slows heart rate (direct action on SA node)Increases force of contraction (inotropic) Increases refractory period at AV node (controls A Fib)Have a low margin of safetyHighly bound to plasma proteinHighly polar
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Dobutamine (Dobutrex)
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Synthetic derivative of isoproterenol – increases heart contractility – decreases tachycardia
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Amrinone
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Bypyridine derivative – inotropic drug
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Sodium channel blockers Quinidine, Procainamide, Lidocaine, Phenytoin
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Act by increasing the effective refractory period (ERP) of depolarized cells – reduces arrhythmias by reducing automaticity in ectopic pacemakers – also have local anesthetic properties
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Beta blockers like propranolol are used to control
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Supraventricular arrhythmias – increase ERP – decrease conduction through AV node
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Bretylium acts to
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Increase the ERP of the atria, ventricle and AV node – used to control life threatening ventricular arrhythmias in the ICU
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Potassium channel blockers work to control arrhythmia
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By prolonging cardiac action potentials
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Calcium channel blockers are used to control
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Supraventricular arrhythmias – depress AV node conduction Verapamil
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Digitalis can control arrhythmias by
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Increasing the AV ERP – prevents ventricular tachycardia in atrial arrhythmias
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K ion preferentially inhibits the
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Automaticity of ectopic pacemakers
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Antiangina drugs Nitrates (nitroglycerine) Calcium channel blockers Beta blockers
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Vasodilation – lowers BP and preload and afterload – decreases oxygen demand (Verapamil, Nifedipine, Diltiazem) – reduce oxygen demand – vasodilation and decrease contractility(Propranolol, Inderal) – lower oxygen demand by decreasing HR – and myocardial contractility
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Fibrinolytic drugs Urokinase Streptokinase
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Convert circulating plasminogen to plasmin to dissolve fibrin clot - used to treat pulmonary emboli Also used to treat coronary thrombosis
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Tissue plasminogen activator (TPA)
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Activates fibrin-bound plasminogen to plasmin – more effective than Streptokinase – fewer side effects
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Antithrombotic drugs block the action of
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Cyclooxygenase – decrease in thromboxane – reduces platelet aggregation – aspirin, ibuprophen, dextran
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Gemfibrozil (Lopid) is used to
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Lower VLDL, LDL and triglycerides – raise HDL Side effects: blurred vision, lens opacities
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Lovastatin (Mevacor, Mevinolin)
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Inhibit HMG CoA reductase – inhibit conversion of HMG CoA to mevalonate (early step in cholesterol synthesis) VLDL, LDL and TRIG decrease, HDL increases Side effects: blurred vision, lens opacities
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Carbonic anhydrase inhibitors (Acetazolamide)
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Decrease bicarbonate and NaCl reabsorption in the proximal tubule – may cause metabolic acidosis
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Osmotic diuretics (Mannitol, Isosorbide)
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Filtered by glomerulus – not reabsorbed due to size so water is excreted with them
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Loop diuretics (Furosemide (Lasix) , Ethacrynic acid)
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Very powerful – short acting – inhibit NaCl transport in the thick ascending loop of Henle – used in acute pulmonary edema
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Thiazide diuretics (Chlorothiazide, Hydrocholothiazide)
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Inhibit Cl reabsorption in the distal tubule – long acting – decrease blood volume and arterial dilation – used in CHF, diabetes insipidus
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Aldosterone antagonist (Spironolactone, Triamterene)
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Weakest diuretic – effects the collecting tubule where aldosetrone functions – potassium sparing
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Benemid (Probenecid) is used to treat
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Hyperuricemia associated with gout
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Anturane
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Increase urinary excretion of uric acid – useful in chronic gout and acute intermittent gout
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Vitamin B1 (Thiamin) def =
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Beriberi – paralysis, heart failure and death
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Vitamin B3 (Niacin) def =
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Pellagra – diarrhea, dermatitis, dementia and death
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Vitamin B6 (Pyridoxine) def =
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Greasy, scaly rash on face and corners or mouth, red sore tongue, mental depression and confusion
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Folate def =
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Megaloblastic anemia
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Vitamin B12 (Cyanocobalamin) def =
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Pernicious anemia
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Vitamin B2 (Riboflavin) def =
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Swollen, inflamed lips with cracks at corners
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Pantothenoic acid is a component of Def =
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Coenzyme A Irritability, restlessness, burning feet
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Biotin acts as a coenzyme in the synthesis of Def =
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Protein and fats Depression, appetite loss, weariness, sleepiness,
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Vitamin C (Ascorbic acid) def =
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Scurvy
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Vitamin A, retinol, retinoic acid, retinal, Beta carotene
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Def = night blindness, mucous membrane abnormalities
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Vitamin D (calciferol) def =
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Rickets, osteomalacia
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Vitamin K def =
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Hemophilia like bleeding disorder
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Vitamin E def =
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Results in abortion of a fetus in females
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Direct acting cholinergic agonists AcetylcholineMethacholineCarbacholPilocarpine
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Applied directly to iris during surgery – short duration Selective activity in cardiovascular systemUsed in POAG – more effective than pilocarpineDirect stimulation on longitudinal muscle of CB, causes follicular conjunctivitis and accommodative spasm** all may precipitate an asthmatic attack through bronchiolar constriction
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Indirect acting cholinergic agonists (anticholinesterase) Reversible PhysostigmineNeostigmineDemecarium Edrophonium (Tensilon) Irreversible Diisopropyl fluorophosphate Echothiophate
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Ung used for POAG at night – antidote is atropine sulfate Antidote for tubocurarine – tx myasthemia gravisUsed topically only for POAG when pilo and carbachol are ineffective – used in management of accommodative esotropiaDrug of choice for the diagnosis of myasthenia gravis aka isofluorophate – may develop iris cysts on the pupillary margin – topical phenylephrine can prevent the development of the cysts may cause anterior subcapsular cataracts, reversible iris cysts
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Phthiriasis palpebrarum tx can be by lid scrubs with
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Physostigmine, echothiophate and isofluorophate
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Cholinergic antagonists AtropineHomatropineScopolamineCyclopentolateTropicamide
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Blick AcH at muscarinic receptors Most potent belladonna alkaloid – antidote is physostigmine
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Adrenergic agaonists NorepinephrineEpinephrine Phenylephrine Hydroxyamphetamine Ephedrine NaphazolineTetrahydrozoline
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CME in aphakic px – initial drug of choice in POAG and ocular HTN – unstable when exposed to light and air – localized deposits with prolonged use In OTC drops to “get the red out” – 1% soln dilates a postganglionis Horner’s syndromeInhibits reuptake of norepi – 1% soln fails to dilate a postgangionlic Horner’s but a preganglionic/central Horner’s dilates normallyTopical vasoconstrictor and decongestant Ocular decongestant and vasoconstrictorOcular decongestant and vasoconstrictor
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Adrenergic antagonists / Beta blocking agents PropranololTimolol
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Blocks both beta 1 and 2 Blocks beta 1 and 2 – more potent than Propranolol – reduces aqueous formation without affecting outflow ** not used in px with respiratory problems
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Adrenergic antagonists / Alpha blocking agents ThymoxamineGuanethidine
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Pheniramine is a drug present in
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Ocular antihistamine preparations
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Inhibit cell wall synthesis PenicillinCephalosporinsCephamycinsBacitracin
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Inhibits transpeptidase Used against G+ and penicillin resistant staph – NOT for G-‘’for G+ only available as an ung
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Disrupt cell membrane permeability Polymyxin B Gramicidine
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For G– doesn’t penetrate an intact cornea – systemically is nephrotoxic – used for infx on lid and conj For G–
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Sulfonamides function by inhibiting bacterial utilization
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Of folic acid
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Sulfonamides are used to treat
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UTIs
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Affect protein synthesis Aminoglycosides Streptomycin Neomycin Gentamicin Tobramycin Others TetracyclinesErythromycinChloramphenicol
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Used to tx aerobic GN bacilli – limited use for GP Bactericidal in high conc. – used to tx TB – may cause vestibular problems, deafness, optic neuritis and renal toxicityBactericidal – broad spectrum – used for topical ocular infx – too toxic when used systemically Bactericidal – broad spectrum – used to tx blepharitis – ototoxic and nephrotoxic – reduced activity when used with chloramphenicolBetter activity against P.aeruginosa – ototoxic and nephrotoxic GN, GP and Chlamydia Active against GPC – used in Staph blepharitis and hordeolumMay cause apalstic anemia – used to tx typhoid fever and other Salmonella infx
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Antivirals that block absorption and penetration Amantidine Idoxuridine
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Influenza A and Rubella HSV keratitis – very toxic
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Antivirals that block DNA polymerase CytarabineVidarabineAcyclovir
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HSV keratitis resistant to Idoxuridine HSV, VZV – neurotoxic and hamatoxicHSV 1, EBV, VZV – carcinogenic, neurotoxic, nephrotoxic
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Antiviral that blocks DNA enzymes Interferons
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VZV,
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Antivirals that block protein synthesis MethisazoneRifampin
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Small pox (variola) virus, vaccinia Topical for vaccinia lesions
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Antifungals Amphotericin BFlucytosineKetoconazoleGriseofulvinNystatinNatamycin
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Binds ergosterol – very toxic Alters fungal RNA – reversal bone barrow suppressionInhibits synthesis of ergosterol The major systemic drug for superficial fungal infx – Topical – binds ergosterol altering membrane permeabilityTopical – low toxicity
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Fluorescein stains the
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Corneal stroma
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Rose Bengal stains
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Dead devitalized epithelial cells
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Carbonic anhydrase inhibitors (CAIs) Acetazolamide (Diamox) Methazolamide (Naptazane) Dichlorphenamide
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Inhibit HCO3 synthesis therefore decreasing aqueous production Used in POAG when topicals do not work alone – causes blood dyscrasias – thrombocytopenia, agranulocyosis – aplastic anemia – may cause myopic shift – metallic taste in mouth – metabolic acidosis Improved intraocular penetration – best tolerated CAI – less acidosis – better for px with lung and kidney problems Causes more confusion and anorexia than other CAIs
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CAIs are all
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Sulfa based
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Iopidine (apraclonidine) is an
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Alpha 2 receptor agonist used to lower IOP
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