Pharmacology - Targets/Mechanism Flashcards

Question

Bupropion

Answer 1

Mechanism unknown Go Fuck Yourself, Sam Rx; depression, smoking cessation, seasonal affective disorder

Answer 2

ACE Inhibitor Angiotensin Converting Enzyme Inhibitor - decreases angiotensin II and aldosterone, increases kinin family (bradykinin) vasodilators [Benazepril, Enalapril, Lisinopril, Quinapril]

Answer 3

Anti-seizure | Blocks Na channels in neuronal membranes

Answer 4

Non-selective adrenoblocker racemic mix; one isomer blocks B1 & B2 non-selectively, the other isomer blocks A1 [Labetalol] Sam loves touching Clay's nuts

Answer 5

echinocandin prototype | inhibitor of Beta(1-3)-glucan synthesis, cell wall component

Answer 6

First Gen Cephalosporin (Get your phd to first, but don't be FAZed by ceFAZolin) beta-lactam, inhibitor of peptidoglycan cross-linking, cell wall synthesis

Answer 7

Third Gen Cephalosporin (Third generations have T in the name) Beta-lactam, inhibit peptidoglycan cross-linking [Cefotaxime, Ceftazidime]

Answer 8

Selective COX-2 In'bitor

Answer 9

Broad Spectrum ABx | inhibits 50s bacterial ribosome

Answer 10

Antimalarial | Binds to hemin, causing dysfunctional cell membranes

Answer 11

Antihistamine first generation H1 blocker | [Diphenhydramine]

Answer 12

Phenothiazine antipsychotic Blocks dopamine receptors in CNS [Fluphenazine, Trifluoperazine]

Answer 13

Antihyperlipidemic bile acid binding resin sequesters bile acids in GI and diverts more cholesterol from the liver to bile acids instead of circulating lipoproteins [Colestipol, Colesevelam]

Answer 14

H2 Blocker on gastric parietal cells ECL cells in gastric mucosa secrete Histamine which binds to H2 receptors on Parietal Cells. H2 are Gs, increase Parietal intracellular cAMP, which stimulates H/K-ATPase to secrete H into stomach lumen. [Ranitidine, Famotidine, Nizatidine]

Answer 15

Second Generation Fluoroquinolone | Bactericidal Inhibitor of DNA gyrase

Answer 16

Antineoplastic - CCNS (Cell cycle non-specific) platinum containing alkylating anticancer drug active against solid tumors (e.g. testes, lung) Adds alkyls to DNA bases (esp. N7 of Guanine), causing abnormal cross-linking and DNA strand breakage. [Carboplatin, Oxaliplatin]

Answer 17

Lincosamide antibiotic | Bacteriostatic 50s ribosomal inhibitor

Answer 18

SERM - selective estrogen receptor modulator | Blocks pituitary estrogen receptors to induce ovulation

Answer 19

Centrally Acting Alpha2 agonist reduces Sympathetic outflow (SANS) and lowers BP [Methyldopa]

Answer 20

Antiplatelet Irreversibly inhibits platelet ADP receptors, prevents expression of gp2a/3b receptors which bind fibrinogen [Ticlopidine]

Answer 21

Indirect sympathomimetic Inhibits norepinephrine transporter (NET) in the presynaptic membrane, increasing synaptic activity of NE [Tricyclic antidepressents act in the same way, also inhibiting dopamine transporter, DAT]

Answer 22

Microtubule assembly inhibitor Reduces macrophage mobility and phagocytosis (Rx: chronic gout)

Answer 23

Antineoplastic, immunosuppressive | Cell Cycle Nonspecific (CCNS) alkylating agent (adds alkyls to DNA bases, causing cross-linking and strand breaks)

Answer 24

Immunosuppressant immunophilin ligand Prevents cytokine production by activated T-Cells; binds to cyclophilin, this complex inhibits calcineurin which regulates nuclear factor of activated T cells (NF-AT), a transcription factor which translocates to the nucleus to increase production of cytokines IL-2, IL-3, & IFNgamma [Tacrolimus, similar, binds FKBP instead of cyclophilin]

Answer 25

Blocks Ca++ release from sarcoplasmic reticulum of skeletal muscle Emergent Rx: Malignant hyperthermia

Answer 26

Vasopressin (ADH) analogue more selective for V2 receptors [Vasopressin] V1: Gq - increase vascular sm contraction V2: Gs - increase H2O perm in collecting tubule (V2 in 2 kidneys)

Answer 27

benzodiazepam prototype binds BZ receptros of the GABAa receptor-chloride ion channel complex facilitates the inhibitory actions of GABA by increasing the FREQUENCY of channel opening [Alprazolam, Lorazepam, Midazolam]

Answer 28

positive inotropic glycoside prototype Inhibits Na/K-ATPase, increasing intracellular Na, which reverses the Na/Ca Exchanger, ultimately increasing intracellular Ca++ --> increased contractility

Answer 29

Antihistamine H1-Blocker [Doxylamine]

Answer 30

Neurotransmitter, agonist at dopamine receptor D1: Gs, relaxes vascular smooth muscle D2: Gi, modulates neurotransmitter release esp. in brain

Answer 31

Antineoplastic Anthracycline drug (Cell-Cycle Nonspecific) intercalates between base pairs to disrupt DNA function, inhibits topoisomerases, forms cytotoxic free radicals [Daunorubicin]

Answer 32

Tetracycline | Bacteriostatic 30s ribosomal protein synthesis inhibitor

Answer 33

Cholinesterase inhibitor | Prevents degradation of acetylcholine by inhibiting cholinesterase, used for myasthenia gravis diagnosis

Answer 34

NNRTI (Nonnucleoside Reverse Transcriptase Inhibitor) | [Delavirdine, Nevirapine]

Answer 35

Antiviral HIV fusion inhibitor synthetic peptide that binds HIV gp41 subunit of the viral envelope, preventing conformational changes required for fusion

Answer 36

Low Molecular Weight Heparin activity against Factor Xa [dalteparin, tinzaparin]

Answer 37

``` COMT inhibitor (Catechol-O-methyltransferase) Acts in the periphery only, prevents conversion of levodopa to 3-O-methyldopa; 3OMD competes with levodopa for transport into CNS and thus decreases effectiveness of levodopa. COMT inhibitors increase CNS levels of levodopa [Tolcapone] ```

Answer 38

Indirect sympathomimetic Displaces stored catecholamines Like amphetamine but with less CNS stimulation and more smooth muscle effects

Answer 39

Adrenoreceptor agonist product of adrenal medulla affinity for all alpha and beta receptors

Answer 40

prolonged vasoconstriction and uterine contraction | [Ergonovine, ergotamine]

Answer 41

Macrolide - No slide - macrolide bacteriostatic protein synthesis inhibitor at 50s [Azithromycin, clarithromycin]

Answer 42

DMARD (disease modifying anti-rheumatic drug) Immunoglobulin based recombinant protein that binds to and inhibits TNFalpha [Infliximab, adalimumab]

Answer 43

Antimycobacterial | inhibitor of arabinogalactan synthesis, a cell wall component, commonly standard part of TB Rx

Answer 44

Anticonvulsant may block T type Ca channels in thalamic neurons Rx Absence seizures

Answer 45

Antihyperlipidemic (EZetimibe-EZglide) | inhibits GI transporter of dietary cholesterol and the cholesterol secreted in bile, inhibits cholesterol uptake in GI

Answer 46

Short-acting opiod agonist | [Remifentanil, sufentanil]

Answer 47

Antiandrogen Steroid inhibitor of 5alpha-reductase that in hibits sythesis of dihydrotestosterone (DHT) [Dutasteride]

Answer 48

Group 1C antiarrhythmic use and state-dependent Na Channel blocker, no effect on action potential duration of QT interval Slow conduction velocity and pacemaker activity

Answer 49

Imidazole antifungal | inhibits ergosterol synthesis, thereby interfering with fungal cell wall permeability

Answer 50

``` Synthetic corticosteroid High mineralocorticoid (Na retention, K/H wasting), moderate glucocorticoid activity (increase glucose and insulin, catabolize proteins, suppress cellular immunity, antiinflammatory cytokines) steroid transported bound to protein, diffuses into cell, binds cytosolic receptor, translocates to nucleus and stimulates tissue-specific gene expression ```

Answer 51

Benzodiazepam receptor antagonist

Answer 52

Antineoplastic, Cell-Cycle Specific (CCS) pyrimidine antimetabolite irreversibly inhibits thymidylate synthase, resulting in dTMP deficiency and a "thymine-less" cell death (uracil is a base, think of deficiency of another base, thymine)

Answer 53

SSRI antidepressent Selective Serotonin Reuptake Inhibitor [citalopram, escitalopram, fluvoxamine, paroxetine, sertraline]

Answer 54

Antiandrogen Androgen receptor antagonist for Prostate Cancer [biclutamide, nilutamide]

Answer 55

Loop diuretic | Inhibits Na/K/2Cl transporter in the thick ascending loop

Answer 56

Anticonvulsant analog of GABA, facilitates the inhibitory action in the CNS Rx partial seizures, bipolar, neuropathic pain

Answer 57

Antiviral | triphosphorylated guanine derivative that causes chain termination (acts at level of DNA polymerase)

Answer 58

Antihyperlipidemic: Fibrate class Activates peroxisome proliferator-activated receptor-alpha (PPARa), a gene regulator, which enhances triglyceride clearance by increasing synthesis of lipoprotein lipase in endothelial cells. In the liver it stimulates fatty acid oxidation (uses them up) which decreases VLDL, and increase apoA1 and A2 production, increasing HDL. Lowers Triglycerides and VLDL, increases HDL.

Answer 59

Aminoglycoside Bacterocidal 30s inhibitor [Tobramycin]

Answer 60

Antidiabetic (GLipizide--GLUCOSE) potent sulfonylrea secretagogue Blocks K channels in pancreatic Beta cells, depolarizing them, causing calcium induced fusion of vesicles and secretion of insulin [Glyburide, repaglinide]

Answer 61

Hormone From pancreatic Alpha cells Increases blood glucose via increased cAMP

Answer 62

Antipsychotic butyrophenone | blocks brain D2 receptors

Answer 63

General Anesthetic volatile (inhaled) halogenated hydrocarbon [isoflurane, sevoflurane]

Answer 64

Anticoagulant large polymeric molecule with activity against thrombin and factor X Antidote: protamine

Answer 65

Antihypertensive arteriolar vasodilator Causes release of endothelial NO which diffuses into smooth muscle cells and stimulates Guanylyl Cyclase to make cGMP, which dephosphorylates Myosin-LC-PO4 to Myosin-LC --> relaxation [Minoxidil]

Answer 66

Thiazide diuretic | blocks Na/Cl transporter in Distal Convoluted Tubule, also stimulates uptake of Ca++

Answer 67

DMARD (disease modifying anti rheumatic drug) antimalarial and T-cell immunosuppressent for rheumatoid arthritis [methotrexate, sulfasalazine]

Answer 68

NSAID | nonselective COX inhibitor with analgesic, antipyretic, and anti inflammatory actions similar to ASA

Answer 69

Carbapenem ABx prototype Bactericidal inhibitor of cell wall synthesis [meropenem, ertapenem]

Answer 70

``` Tricyclic antidepressent Blocks the reuptake of 5-HT and NE Similar to SNRIs but with broader peripheral effects (SNRIs are more selective) [amitriptyline, clomipramine, doxepin] ```

Answer 71

Antiviral HIV protease inhibitor Inhibits the protease which is essential for cleaving HIV proteins into proper length/configuration [amprenavir, nelfinavir, ritonavir, saquinavir]

Answer 72

Highly potent NSAID | Rx for neonatal PDA or acute inflammatory rxn (e.g. gout)

Answer 73

Antimuscarinic aerosol for asthma competitively block muscarinic receptors in the airway, effectively preventing bronchoconstriction from vagal discharge [Tiotropium]

Answer 74

antimycobacterial structurally similar to pyridoxine (vit B6) Mechanism involves inhibition of mycolic acid, a characteristic component of mycobacterial cell walls. Must be activated by a tubercular enzyme, and then targets a different enzyme, thus there is double opportunity for resistance.

Answer 75

Beta agonist, B1 & B2 | Bronchodilator, cardiac stimulant

Answer 76

Antihelminthic | intensifies GABA mediated neurotransmission in nematodes, no access to human CNS

Answer 77

Antifungal azole prototype Inhibits synthesis of ergosterol interferes with fungal cell membrane permeability by preventing ergosterol synthesis, acting at the step of 14alpha-demethylation of lanosterol [fluconazole, itraconazole, voriconazole]

Answer 78

NSAID | mainly used as a systemic analgesic

Answer 79

3TC Nucleoside reverse transcriptase inhibitor (NRTI) Triphosphorylated nucleoside that competitively inhibits binding of dNTP-binding site of reverse transcriptase AND cause chain terminators via insertion into growing DNA chain

Answer 80

Antiepileptic rate-dependent Na channel blocker, prolongs the inactivated state of Na channel, increasing refractory period of neuron Absence and partial seizures

Answer 81

Prostaglandin F, topically for closed angle glaucoma

Answer 82

Direct thrombin inhibitor recombinant form of medicinal leech protein, directly inhibits thrombin (LEpirudin --> LEECH)

Answer 83

GnRH analog | continuous therapy down regulates receptor expression, decreasing gonadotropins and gonadal hormone synthesis

Answer 84

Dopamine precursor | converted to dopamine in CNS

Answer 85

``` Respiratory Fluoroquinolone -Ololol gyrating DNA gyrase -oxacins - Flocks of sinners Bactericidal inhibitor of DNA gyrase Other resp fluoro's: gemifloxacin, moxifloxacin ```

Answer 86

Progestin used for contraceptives thickens cervical mucus, inhibits sperm motility, thins endometrium

Answer 87

Amide local anesthetic highly selective use-dependent group 1B antiarrhythmic Little effect on normal cardiac cells, shortens AP duration, no change on ECG (because doesn't affect normal cells) nerve block and acute post-MI ischemic ventricular arrhythmia

Answer 88

Antimanic | Blocks recycling of the phosphatidylinositol second messenger system

Answer 89

Second gen Antihistamine | H1 blocker, less CNS pen

Answer 90

ARB Angiotensin receptor blocker (AT1 receptor blocker) Prevents the effects of RAA System, decreases blood pressure

Answer 91

statin - antihyperlipidemic HMG-CoA Reductase Inhibitor Inhibits the rate-limiting step of cholesterol synthesis in hepatocytes, prevents converstion of HMG-CoA to mevalonate, thus decreasing the hepatic pool of cholesterol. In response, the liver upregulates high affinity LDL receptors and clears LDL and VLDL from the blood [atorvastatin, fluvastatin, pravastatin, rosuvastatin, simvastatin]

Answer 92

Osmotic diuretic fluid pulled osmotically into the renal tubules Rx for high ICP and promote excretion of renal toxins in hemolysis/rhabdo

Answer 93

Antihelminthic Rx for nematode infection inhibits microtubule synthesis and glucose uptake in nematodes [Albendazole, thiabendazole]

Answer 94

Progestin (Depo-Provera) | used in combination with an estrogen for menopause or long acting injection

Answer 95

Antimalarial Mechanism unknown Go fuckity fuck yo' self!

Answer 96

Opioid analgesic Strong agonist at mu opioid receptors, blocks muscarinic receptors, some serotonergic activity Equivalent to morphine, but orally available

Answer 97

Oral antidiabetic prototype Biguanide inhibits hepatic and renal gluconeogenesis through a poorly understood mechanism which involves activation of an AMP-stimulated protein kinase

Answer 98

Opioid | synthetic mu agonist, orally available morphine

Answer 99

Antithyroid - small sulfur containing thioamide blocks peroxidase-catalyzed iodination of the tyrosine residues of thyroglobulin and coupling of DIT and MIT. Little peripheral inhibition of conversion of T4 to T3 (Propylthiouracil inhibits peripheral conversion) [Propylthiouracil]

Answer 100

Antineoplastic, immunosuppressant, DMARD Cell Cycle-Specific inhibitor of dihydrofolate reductase. This prevents synthesis of Tetrahydrofolate (THF), which is a necessary intermediary for both protein and purine nucleotide synthesis, interfering with nucleic acid and protein metabolism

Answer 101

Antihypertensive | prodrug of methylnorepinephrine, a CNS-active alpha2 agonist, reducing SANS outflow from vasomotor center

Answer 102

Prokinetic | Dopamine D2 agonist used to stimulate upper GI motility in patients with gastroparesis, also antiemetic

Answer 103

Antiprotozoal antibiotic Interferes with nucleic acid synthesis after undergoing a reductive bioactivation of their nitro group by ferrodoxin (present in anaerobic parasites) to form reactive cytotoxic products [Tinidazole]

Answer 104

The Stone of Mephistopheles Medical abortion in early pregnancy, with misoprostol Progestin and glucocorticoid receptor antagonist

Answer 105

Prostaglandin E1 derivative, prevents GI ulcers by NSAIDs | abortifacient with mifepristone (the stone of mephistopheles)

Answer 106

Leukotriene receptor blocker (esp. LTD4) used for prophylaxis in asthma [Zafirlukast]

Answer 107

Yum. | Mu opioid receptor agonist.

Answer 108

Penicillinase-resistant penicillin Beta-lactam antibiotic, inhibits peptidoglycan cell wall cross-linking bactericidal [methicillin, oxacillin, cloxacillin, dicloxacillin]

Answer 109

Opioid mu receptor antagonist | Antidote for opioid overdose

Answer 110

Cholinesterase inhibitor synthetic quaternary nitrogen carbamate with little CNS effect Carbamate binds to Cholinesterase and is immediately hydrolyzed, but the remaining ion portion of neostigmine is slow to dissociate from cholinesterase, thus preventing it from hydrolyzing acetylcholine. [Pyridostigmine, physostigmine]

Answer 111

Vitamin B3 In liver, niacin reduces VLDL synthesis. In adipose tissue it activates a signaling pathway that reduces hormone-sensitive lipase activity, lowering plasma fatty acid and triglyceride levels. Reduces catabolism of HDL Also apparently decreases circulating fibrinogen and increases tpa

Answer 112

Dihydropyridine Ca Channel Blocker prototype blocks voltage-gated L-type calcium channels, this decreases intracellular Ca++, reducing muscle contractility and dilating blood vessels [amlodipine, felodipine, nicardipine]

Answer 113

Endogenous vasodilator released from vascular endothelium stimulates guanylyl cyclase to make cGMP, which favors dephosphorylation of MLC-PO4 to MLC, which prevents crossbridging and contraction

Answer 114

Antianginal vasodilator releases NO in veins (less in arteries), causing sm dilation Decreases preload, which decreases wall tension and thus cardiomyocyte oxygen demand [isosorbide dinitrate, isosorbide mononitrate]

Answer 115

Alpha 1 and 2 agonist, Beta 1 agonist | vasoconstrictor

Answer 116

Atypical Antipsychotic High affinity antagonist at 5-HT2a receptorts (as opposed to typical antipsychotics which block D2 receptors) Blocks positive and negative effects of schizophrenia, few extrapyramidal side effects [Quetiapine, risperidone, sertindole, clozapine]

Answer 117

PPI Irreversible blocker of H/K ATPase propton pump in gastric parietal cells [Esomeprazole, dexlansoprazole, lansoprazole, pantoprazole, rabeprazole]

Answer 118

5-HT3 receptor blocker antiemetic [Dolasetron, granisetron, palonosetron]

Answer 119

Antiviral Neuraminidase inhibitor prevents release of mature virions of Influenza A and B

Answer 120

Anti Muscarinic muscarinic cholinoceptor blocker [Tolterodine]

Answer 121

``` Antineoplastic Plant alkaloid Cell Cycle Specific (M phase) Inhibits mitotic spindle disassembly into tubulin monomers [Docetaxel] ```

Answer 122

Chelator, Bidendate chelator forms two bonds to Copper ion, prevents it from interacting with anything else, easily excreted (water soluble); PCN derivative Rx: Copper Poisoning/Wilson's

Answer 123

IV PCN | Inhibits stage III cell wall synthesis, preventing peptidoglycan cross-linking.

Answer 124

Irreversible non selective MAOI Monoamine Oxidase A metabolizes NE & 5HT, MAO B metabolizes Dopamine. Action in Presynaptic axon terminal. Inhibition of metabolism of neurotransmitters leads to increased neurotransmitter storage in vesicles, which results in great amount release into the synaptic cleft.

Answer 125

Barbituate Facilitates GABA-mediated neuronal inhibition by increasing DURATION of channel opening. May block excitatory neurotransmitters

Answer 126

Irreversible alpha blocker Covalently binds to alpha-receptor, non-competitively and irreversibly blocking its activity [Phentolamine]

Answer 127

Anticonvulsant Blocks Na+ channels in neuronal membranes, preventing or slowing depolarization Tonic-Clonic or Partial Seizures

Answer 128

Muscarinic direct acting partial agonist Increase parasympathetic response M receptors are Gq (M1, M3, M5) and Gi (M2, M4) which will increase DAG/IP3 and cause sm contraction via Ca++ release, and inhibit Adenylate Cyclase, decreasing cAMP and releasing inhibition MLCK, causing sm contraction

Answer 129

Extended spectrum PCN with pseudamonas aeruginosa coverage

Answer 130

Acetylcholinesterase regenerator Antidode (with Atropine) for organophosphate poisoning. Oxime moiety with extremely high affinity for phosphorus in organophosphates, displaces them from the active site of acetylcholinesterase enzyme active site, thus regenerating the enzyme. Essentially an indirect anticholinergic

Answer 131

Dopamine D3 agonist in CNS first line for parkinsonism [ropinirole, bromocripine (which is more toxic)]

Answer 132

Antihelminthic Increases tematode and cestode (fluke and tapeworm) membrane permeability to Ca++, causing muscle contraction followed by paralysis. [Albendazole, which sounds like a wizard's name. Albendazole the Aberration Slayer.]

Answer 133

Alpha1-selective blocker for HTN and BPH [terazosin, doxazosin, Tamsulosin (only for BPH)]

Answer 134

Short acting, potent glucocorticoid Steroid (S) carried in blood by corticosteroid binding globulin (CBG), S enters cytoplasm and binds receptor which is stabilized by heat-shock protein 90 (HSP90). HSP90 is released, S-Receptor complex forms dimer and enters nucleus to bind glucocorticoid response element (GRE) which alters gene transcription. New mRNA is synthesized, exported to cytoplasm, protein is translated that has ultimate effect.

Answer 135

Uricosuric Normally 90% of uric acid filtered at kidney is reabsorbed in the proximal tubule, probenecid is a weak acid that competes for reabsorption by the weak acid transport mechanism, thereby increasing uric acid excretion (Low doses it competes with uric acid for secretion into tubule so may actually increase uric acid concentration) PCNs (and others?) are secreted into the nephron tubule, but this action is inhibited by Probenecid, increasing the half-life. (Presumably via the same general mechanism, a competitive weak acid, that is it competes with PCN for secretion into the tubule)

Answer 136

Group 1A antiarrhythmic Sodium channel blocker, prolongs the AP duration (see below), slows conduction velocity in atria, purkinje fibers and ventricular cells, some specificity for ischemic tissue but not as much as 1B antiarrhythmics, may abolish abnormal pacemakers if they depend on sodium channels. Use Dependent Group 1A's prolong QT because they have some effect on Potassium current, even though they are considered Sodium Channel blockers. This is why they prolong the AP. [quinidine]

Answer 137

Non-selective Beta Blocker

Answer 138

PGI2, endogenous prostaglandin vasodilator and inhibitor of platelet aggregation (opposite effect of TXA2) Selective COX-2 inhibitors believed to preferentially inhibit PGI2 over TXA2, leading to thrombotic risks [epoprostenol, analog used for primary pulm. HTN]

Answer 139

Antiprotozoal antifolate that inhibits DHF reductase and is synergistic, via sequential blockade, with sulfadiazine against Toxoplasma gondii Supplement with Folinic acid to offset hematologic tox

Answer 140

Antimalarial Plasmodium undergo primary dev. stage in liver, then parasitize erythrocytes. Quinine is a blood schizonticide, meaning it only affects parasitic forms found in RBCs. Prevents separation of dsDNA, thus inhibiting genome replication and transcription of mRNA

Answer 141

Hypnotic Agonist at brain melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus, for use when onset of sleep is delayed (decreases latency of sleep onset) Believed to have no abuse potential because no GABA-ergic effect. Sounds like the name of a Sorcercer. Ramelteon, the Enchanter, will hypnotize you and put you to sleep.

Answer 142

AntiHTN selective inhibitor of vesicle catecholamine-H+ antiporter (VMAT) rarely used anymore

Answer 143

Antimicrobial Part of TB regimen (RIPE, Rifampin, Isoniazid, Pyrazinimide, Ethambutol) CYP450 Inducer Inhibitor of DNA-dependent RNA polymerase [Rifabutin]

Answer 144

``` Navir tease a protease Antiviral HIV protease inhibitor (protease cleaves virally encoded proteins to make mature, active virions), often added in low dose combination therapy for AIDS to inhibit metabolism of other drugs CYP450 In'bitor [Indinavir] ```

Answer 145

Oral antidiabetic Thiazoldinedione stimulator of peroxisome proliferator-activator gamma nuclear receptors (PPARgamma). Binds nuclear receptor and regulates transcription of genes encoding proteins involved in carbohydrate metabolism. Increases tissue sensitivity to insulin. Increases uptake of glucose in adipose and muscle, inhibits hepatic gluconeo, reduces fasting and postprandial hyperglycemia. [pioglitazone]

Answer 146

Is a Dragon's name if I've ever heard one. Rivaroxaban, The Blood Drinker, The Sanguine Scourge, The Tenth Wonder of the World (after King Kong (8th) and the Loch Ness Monster (9th)). Factor X inhibitor, prevention of DVT, PE, postsurg thromboembolism, and stroke in A. Fib

Answer 147

MAO-B inhibitor Selectively inhibits MAO-B, which metabolizes Dopamine, thus no tyramine interaction at normal doses. Increases vesicular concentration of Dopamine for greater release after neuronal stimulation. Rx for Parkinson's. [Rasagiline]

Answer 148

PDE-5 inhibitor Phophodiesterase-5 breaksdown cyclic guanosine monophosphate (cGMP). cGMP dephosphorylates Myosin-LC-PO4 to Myosin-LC, which promotes vasodilation and smooth muscle relaxation. Inhibition of PDE-5 thus prolongs the effects of cGMP, increasing vasodilation [Tadalafil, vardenafil]

Answer 149

Group 3 Antiarrhythmic (Potassium Channel Block) Chiral compound, both isomers block Potassium Channels, and one isomer blocks the beta receptor also. Slows repolarization, increasing the refractory period and causes visible ECG changes including: Increased PR interval and especially a PROLONGED QT

Answer 150

K+-Sparring Diuretic Aldosterone receptor antagonist Blocks aldo receptor, prevents synthesis and insertion of ENaC into the membrane in Distal Tubule. Also blocks Androgen receptor, thus Rx for hirsutism. Eplerenone is more selective aldosterone antagonist, with less anti-androgen receptor effects

Answer 151

BacteriCIDAL protein synthesis inhibitor antibiotic (most prot. synth. inh.'s are static) Bind to 50s subunit and constricts exit pore, also decreases tRNA synthetase activity so there is less tRNA in the cell for protein synthesis. Synercid is a combination of quisupristin and dalfopristin Used for resistant MRSA, VRE and pneumococcus [Linezolid, similar use/spectrum, binds 50s, bacterioSTATIC, different class (Oxazolidinone)]

Answer 152

Depolarizing neuromuscular relaxant Nicotinic agonist that depolarizes the NMJ, after initial twitches and fasciculations the muscle relaxes because it is unable to repolarize (necessary for subsequent depolarizations). With continuous infusion, there is a change in the mechanism, it switches from preventing repolarization to increasing resistance to depolarization. No antidote. Risk for Malignant Hyperthermia (Rx Dantrolene)

Answer 153

Prodrug metabolized to sulfapyridine and 5-aminosalicylic acid (5-ASA, also known as mesalamine). The sulfapyridine is added to decrease absorption in small intestine, allowing 5-ASA to reach the large intestine where it has topical anti-inflammatory effect, the exact mechanism of which is unknown (perhaps interfering with T Cells or Prostaglandins) The Sulfapyridine is considered responsible for the systemic adverse effects. [Mesalamine, balsalazide, olsalazine]

Answer 154

5-HT,1d receptor agonist for aborting migraines 5-HT,1d is Gi (decreased cAMP); in the brain it mediates synaptic inhibition via increased potassium conductance [other -triptans]

Answer 155

SERM (selective estrogen receptor modulator) Rx ER positive breast cancer Antagonist at breast ER, agonist at endometrial ER, thus carries increased risk of endometrial cancer. [Toremifene] [Raloxifene - SERM for osteoporosis, agonist in bone, antagonist at breast and endometrium]

Answer 156

Antifungal - alters cell membrane permeability Fungicidal inhibitor of squalene epoxidase, leads to accumulation of squalene, which is toxic because it interferes with ergosterol synthesis. Ergosterol is a sterol specific to fungal cell membranes most effective for onychomycosis

Answer 157

Bacteriostatic Antibiotic Inhibition of protein synthesis. Binds to 30s subunit, prevents incoming binding of charged tRNA to the A site. [Doxycycline, tigecycline]

Answer 158

Bronchodilator A naturally occuring methylxanthine found in tea that inhibits PDE. The increased cAMP inhibits myosin-LC kinase, leading to smooth muscle relaxation and bronchiodilation. [caffeine (coffee), theobromine (cocoa)]

Answer 159

Bactrim Synergistic sequential blockade of Folate Synthesis. Normally p-Aminobenzoic acid (PABA) is converted to dihydrofolate by dihydropteroate synthase, and DHF is converted to THF by dihydrofolate reductase. Sulfonamides (like SMX) are structurally similar to and compete with PABA, thus inhibiting the action of dihydropteroate synthase, preventing formation of DHF, and trimethoprim inhibits dihydrofolate reductase, preventing conversion of what DHF is formed to THF. SMX ----| dihydropteroate synthase (----| DHF) TMP ----| dihydrofolate reductase (----| THF)

Answer 160

Non-depolarizing paralytic competitive nicotinic blocker at NMJ [pancuronium, atracuronium, vecuronium, other -curiums or -oniums]

Answer 161

Indirect sympathomimetic | releases or displaces NE from stores in nerve endings

Answer 162

Anticonvulsant Treats ALL the seizures, and acts by ALL the mechanisms! Na+ Channel Blockade: rate-dependent prolongation of inactive state (decreased excitation) GABA effects: VA inhibits GABA aminotransferase (GABA-T) which terminates the GABA activity (increased inhibition) Ca++ Channel Blockade: blocks T-type low threshold thalamic Ca++ channels (decreased rhythmic D/C, Rx: abscence seizures) Other: neuronal membrane hyperpolarization by enhanced K+ channel permeability (both decreased excitation and increased inhibition)

Answer 163

Bactericidal Antibiotic | Inhibits stage 2 cell wall synthesis by binding D-ala D-ala and preventing polymerization of glycoproteins

Answer 164

L-Type Calcium Channel Blocker Vasodilator and antiarrhythmic at the AV node State and use dependent selective depression of calcium channel activity AV conduction velocity decreased, effective refractory period increased and increased PR interval on ECG [Diltiazem, nifedipine]

Answer 165

Antineoplastic Cell Cycle Specific (M Phase) Inhibits mitotic spindle formation by blocking tubulin dimers from forming microtubules [vinblastine]

Answer 166

Oral Anticoagulant Inhibitor of Vitamin K Epoxide Reductase (VKOR), which converts vitamin K epoxide to reduced vitamin K, which is used for postranslational modifaction of clotting factors X, IX, VII, and II Antidote: Vit K (takes 6-8 hrs), fresh plasma (for acute Rx)

Answer 167

Antiviral NRTI, nucleoside reverse transcriptase inhibitor, lacks a 3' -OH, so when incorporated into DNA synthesis, it causes chain termination [abacavir, didanosine (ddI), lamivudine (3TC), stavudine (d4T), zalcitabine (ddC)]

Answer 168

Nonbenzo hypnotic acts at BZ1 receptor subtype and is reversed by flumazenil [Zaleplon, eszopiclone]

Pharmacology - Targets/Mechanism Flashcards

(192 cards)