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191 Cards in this Set

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