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U World > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Trastuzumab

A

Monoclonal Antibody used in the treatment of breast cancer

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2
Q

Griseofulvin

A

Enters fungal cells, binds microtubules, and inhibits mitosis, effective only against dermatophyte fungi, as it accumulates, in keratin containing tissues.

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3
Q

Echinocandins (Caspofungin and Micafungin)

A

Suppress the synthesis of cell wall by blocking gluten synthesis (1,3-beta-D-glucan is a major polysaccharide component of the fungal cell wall) Caspofungin is most active against cryptococcus neoformans and has limited activity against Mucor and Rhizopus species.

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4
Q

Enoxaperin

A

Form of low molecular weight of heparin that functions by binding and activating antithrombin 3 which binds to factor Xa and stops it from converting prothrombin to thrombin. Less thrombin results in anti-coagulent effect.
Shown to cause significant reduction in death and recurrent myocardial infarction as compared with unfractional heparin.

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5
Q

Valproate

A

Blocks voltage gated sodium channels and enhances GABA synthesis and release. As an anticonvulsant, it is used for generalized tonic clonic seizures, it is drug of choice for myoclonic seizures and second line agent for absence seizures. As a mood stabilizer it is used in acute mania and maintenance of bipolar disorder, especially in patients with rapid cycling (>4 episodes per year) and episodes with mixed manic depressive features.
Side effects include hepatotoxicity and neural tube defects.

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6
Q

Acyclovir

A

Used for confusion and seizures. Can cause crystalline nephrotoxicity if adequate hydration is not also provided. When its concentration exceeds its solubility in collecting duct, crystallization, crystalluria and renal tubular damage may result.

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7
Q

Abciximab

A

Chimeric mouse human antibody against the platelet GpIIb/IIIa receptor. Blocks final step in platelet aggregation. Administered during angioplasty in patients with acute coronary syndrome.

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8
Q

Imatinib

A

Diagnosis of CML requires the presence of the Philadelphia chromosome or the BCR/ABL fusion gene. It is a potent inhibitor of the BCR/ABL protein tyrosine kinase. It inhibits the cellular proliferation of BCR/ABL expressing cells without inducing apoptosis. ORAL Medications used for management of CML.

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9
Q

Interleukin-2

A

Cytokine that regulates the activation and differentiation of T cells to aid in tumor cell destruction. Used for treatment of renal cell carcinoma and melanoma.

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10
Q

Infliximab

A

Chimeric (human/murine) IgG1 monoclonal antibody to TNF-œ. Used in management of rheumatoid arthritis and treatment of ankylosing spondylitis and fistulizing Crohn’s disease.

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11
Q

Rituximab

A

Biologic response modifier (BRM) intended to restore or induce the immune system’s ability to overcome disease. Monoclonal antibody used in lymphoma immunotherapy that specifically targets CD20 surface immunoglobulin.

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12
Q

Fluoxetine

A

Serotonin reuptake inhibitor (SSRI) used for panic disorder, social phobia, generalized anxiety disorder and OCD. Sexual dysfunction may limit their use.

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13
Q

Alprazolam

A

Benzodiazepine with onset of action of 1-2 hours and a relatively short half life. It is used on an as needed basis

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14
Q

Buspirone

A

Selective agonist of 5HT(1A) receptor, safe and effective treatment for generalized anxiety disorder, clinical response is often delayed for up to 2 weeks of regular use. Not effective when used on an as needed basis, dependence does not occur with chronic treatment

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15
Q

Terbinafine

A

Accumulates in skin and nails and is used to treat dermatophytosis. Inhibits ultimately results in decreased synthesis of ergosterol.

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16
Q

Eplerenone

A

New aldosterone antagonist that has fewer side effects than spironolactone and is often used in those that cannot tolerate spironolactone. Side effect is gynecomastia in 1% of patients. Aldosterone causes resorption of sodium and water and wasting of potassium and hydrogen ions at the distal portion of the nephron leading to hypokalemia and alkalosis.

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17
Q

Spironolactone

A

First line drug for primary hyperaldosteronism (Conn’s Syndrome) caused by aldosterone secreting tumor (adenoma). Patient presents as hypertensive, hypokalemic, metabolic alkalosis, and decreased plasma renin activity. Side effect includes gynecomastia in 9% of patients. Addition of low dose spironolactone to standard therapy (ACEIs, digoxin, diuretic) significantly reduced morbidity and mortality in class 3 and 4 heart failure patients.

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18
Q

Organophosphates

A

Lipid soluble and thus are readily absorbed via oral cutaneous and inhalation routes of exposure. Readily penetrate blood brain barrie and induce CNS symptoms. They are irreversible cholinesterase inhibitors; elicit cholinergic stimulation that lasts until new cholinesterase enzymes are synthesized. Poisoning is treated with muscarinic antagonists like atropine in addition to pralidoxime, a cholinesterase enzyme reactivate. Patient presents with non focal neurological deficits, confusion mitosis, bradycardia, relatively low BP, cutaneous vasodilation (flushing) diaphoresis, lacrimation and bronchospasm.

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19
Q

Loop diuretics

A

Work in the loop of hence and inhibit sodium resorption but the kidney is still able to absorb some sodium in the distal convoluted tubule and does not have increased absorption in the proximal tubule.

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20
Q

Thiazide Diuretics

A

Work in the distal convoluted tubule and impair sodium resorption. As a result the kidney eventually tries to compensate by increasing sodium in the proximal tubule. Presently are the first line treatment for essential hypertension in outpatient setting.

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21
Q

Sertraline

A

SSRI, indicated in treatment of major depression, OCD, and anxiety disorders.

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22
Q

Olanzapine

A

Second generation antipsychotic used to treat psychotic and mood disorders. Side effects, include weight gain and increased risk of metabolite syndrome (dyslipidemia, hypertension, and hyperglycemia)

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23
Q

Lorazepam

A

Benzodiazepine, enhances the affinity of GABA for its receptor (increases the frequency of chloride channel openings) thereby increasing its inhibitory potential. First line medication for treatment of active seizures acute anxiety and alcohol withdrawal.

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24
Q

Ethosuximide

A

Anticonvulsant, drug of choice for absence seizures. Reduces Ca+ currents in T-type Ca+ channels in the neurons thereby inhibiting the propagation of action potentials.

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25
Q

Lithium

A

Mood stabilizer that is effective in the acute and maintenance treatment of bipolar disorder. Modifies second messenger signal transduction (e.g.. adenyl cyclase and phospho-inositol pathways) resulting in decreased excitatory neurotransmission. Side effects include diabetes insipidus, hypothyroidism, tremor, ebstein’s anomaly. Has a very narrow therapeutic index. Almost exclusively excreted by the kidneys with filtration and absorption in the proximal tubules following sodium reabsorption. Renal injury, toxins, and drugs that lead to proximal tubular absorption of Na+ (NSAIDS, ACE inhibitors and diuretics) also increase levels and increase lithium toxicity

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26
Q

Lamotrigene

A

Effective in depressed phase of bipolar disorder and is associated with skin rash which can rarely progress to life threatening mucocutaneous reactions. Stevens Johnson Syndrome. Also indicated for focal seizures.

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27
Q

Carbamazepine

A

Used as mood stabilizer in bipolar disorder, effective in treatment of mania, it is a CYP450 inducer that can cause lower levels of concomitant medications. Manic episode maintenance, absence, generalized tonic clonic, myoclonic seizures. Side effects include agranulocytosis, hyponatremia (SIAHD) neural tube defects.

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28
Q

Flucytosine

A

Inhibits the synthesis of both DNA (replication) and RNA (protein synthesis) in fungal cells. Mainly used as a synergistic agent with amphotericin B, particularly in the treatment of cryptococcal meningitis.

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29
Q

Amphotericin B

A

A polyene anti fungal that binds ergosterol in the fungal cell membrane and leads to pore formation and cell lysis

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30
Q

Itraconazole

A

an azole anti fungal that inhibits ergosterol synthesis

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31
Q

Bosentan

A

An endothelin receptor antagonist that blocks the effects of endothelin (a potent vasoconstrictor that also stimulates endothelial proliferation). It decreases pulmonary arterial pressure and lessens the progression of vascular and right ventricular hypertrophy.

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32
Q

Clopidogrel

A

Inhibits ADP induced platelet aggregation. It is used in atherosclerotic ischemic disease and to prevent acute stent thrombosis following precutaneous coronary interventions.Irreversibly blocks the platelet surface ADP receptors essential for platelet activation, aggregation and fibrin binding. Used as an alternative in patients with allergic reaction to aspirin.

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33
Q

Enalapril

A

An angiotensin converting enzyme inhibitor. It is used for treatment of congestive heart failure, hypertension, and diabetic nephropathy.

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34
Q

Etanercept

A

Inhibits tumor necrosis factor (TNF) activity by competitively binding to TNF and preventing it from interacting with cell surface receptors. It is an anti inflammatory agent used for treatment of rheumatoid arthritis, psoriasis, and psoriatic arthritis.

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35
Q

Indomethacin

A

A nonspecific cyclo-oxegenase inhibitor that suppresses prostaglandin synthesis, it is used as an anti-inflammatory agent and pain reliever.

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36
Q

Piperacillin-Tazobactam

A

Tazobactam is a beta lactamase inhibitor (an enzyme that breaks down penicillin). Piperacillin is an extended spectrum penicillin. The combination of the two is effective against a large number of Gram (+) and Gram (-) and anaerobic bacteria.

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37
Q

Ciprofloxacin

A

1st gen fluoroquinolone that acts by interfering with bacterial topoisomerase 2 (DNA gyrase). It is active against most gram negative rods and bacilli, including Legionella and P. aeruginosa. It is not effective for anaerobic infections.

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38
Q

Ceftriaxone

A

3rd gen parenteral cephalosporin. It is active against Gram (-) bacilli, including most of the enteric organisms: H. influenza, Klebsiella pneumoniae, Neisseria, and Serratia species. It has poor activity against anaerobes. Used in septic arthritis due to gonococcus.

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39
Q

Azithromycin

A

Macrolide antibiotic that binds to the 50S subunit of bacterial ribosomes, thereby inhibiting protein synthesis. It is used for chlamydia, mycoplasma species, H. influenza, Moraxella catarrhalis infections.

40
Q

Vancomycin

A

A tricyclic glycopeptide that inhibits the synthesis of peptidoglycan, which is a main component of the cell wall of gram positive bacteria. It is used against methicillin resistant S. aureus and S. epidermidis as well as C. difficile.

41
Q

6 Mercaptopurine

A

Used for maintenance of remission of ALL. Like 6 thioguanine it is a cytotoxic purine analog that inhibits de novo purine synthesis after being converted to active form by HGPRT. Degradation of these agents to inactive metabolites is done by Xanthine oxidase and thiopurine methyltransferase in the liver. Chemotherapy must be reduced by 75% if used with XO inhibitor Allopurinol.

42
Q

Methotrexate

A

Inhibits dihydrofolate reductase thereby blocking the conversion of dihydrofolate to tetrahydrofolate and disrupting the synthesis of thymidine and purines.

43
Q

Nimodipine

A

Calcium channel blocker, has been shown in studies and reviews to decrease morbidity and mortality due to cerebral vasospasm when used as a preventive agent following subarachnoid hemorrhage. It is identified as cerebral selective drug, though it is unclear whether the mechanism of its cerebral protection is due to vasodilation or neural protection.

44
Q

Beta adrenergic blockers

A

i.e metoprolol, serve to decrease the heart rate and blood pressure.

45
Q

Central Sympatholytics

A

i.e. methyldopa and clonidine, stimulate alpha-2A receptors centrally which causes a decrease in generalized sympathetic outflow. This would cause a decrease in blood pressure in addition to other effects of decreasing both alpha and beta sympathetic stimulation.

46
Q

Osmotic diuretics

A

i.e. Mannitol, are part of the treatment for increased intracranial pressure.

47
Q

ACE inhibitors

A

i.e captopril, lisinopril, and enalapril decrease BP and cardiac hypertrophy by inhibiting the conversion of Angiotensin 1 and Angiotensin 2. They are useful in hypertension, prevention of diabetic nephropathy, and in heart failure with systolic dysfunction. Their major side effects include cough and angioedema.

48
Q

Nitrates

A

i.e. nitroglycerin and isosorbide mononitrate are used as vasodilators primarily for the treatment of angina pectoris

49
Q

Isoproterenol

A

Increase cardiac contractility by acting on myocardial beta 1 adrenergic receptors. In lower doses it selectively binds to beta 2 receptors causing relaxation of vascular smooth muscle. It has negligible effects on alpha receptors.

50
Q

Norepinephrine

A

Acts on alpha 1 receptors causing an increase in systemic vascular resistance. Can also act as a weak agonist at beta 1 receptors potentially increasing myocardial contractility.

51
Q

Clonidine

A

A central sympatholytic agent which decreases peripheral vascular resistance and heart rate by activating alpha 2 adrenergic receptors in the brainstem.

52
Q

Labetalol

A

A non selective beta blocker that also has alpha 1 receptor blocking effects. Both myocardial contractility and systemic vascular resistance would decrease with this.

53
Q

Phenylephrine

A

Sympathomimetic drug with alpha 1 > alpha 2 agonist effects. Infusion of this drug would increase systemic vascular resistance.

54
Q

P450 inducers

A

Decrease concentration of phenytoin in plasma and diminishes its effectiveness. Examples are barbiturates, phenytoin, rifampin, carbamazepine, griseofulvin, and chronic alcohol consumption.

55
Q

P450 inhibitors

A

Slow hepatic metabolism, which increases the toxicity of P450 inducers like phenytoin. Examples are isoniazid, cimetidine, macrolides, azole antifungals, and grapefruit juice.

56
Q

Fluconazole

A

Triazole class anti fungal used to treat candidiasis, cryptococcosis, histoplasmosis, blastomycosis, and coccidioidomycosis.

57
Q

H1 receptors

A

Found in the vascular endothelium and bronchial smooth muscle where they help to mediate vascular permeability and bronchoconstriction respectively.

58
Q

H2 receptors antagonists

A

Used to block gastric acid secretion by parietal cells.

59
Q

Nicotinic cholinergic receptors

A

Found on postganglionic neurons in sympathetic and parasympathetic ganglia and on skeletal muscle cells at the neuromuscular junction. Drugs such as tubocurarine that block these receptors are often used during general anesthesia to induce paralysis. Adverse effects associated with these agents include respiratory paralysis and autonomic ganglionic blockade that can cause hypotension and tachycardia.

60
Q

alpha 1 - adrenergic agonists

A

sometimes given to patients with allergic rhinitis because their vasoconstrictive action helps to alleviate nasal congestion. These agents cause mydriasis if administered intraocularly or in large systemic doses.

61
Q

Hydrochlorothiazide

A

A thiazide diuretic that works by blocking Na-Cl symporters in distal convoluted tubule resulting in enhanced Na, Cl, and water excretion. Since only a small amount of Na reaches distal tubules, thiazides are not as efficacious diuretics as loop diuretics and are seldom used in treating congestive heart failure. However, in diuretic resistant patients, thiazides and thiazide like diuretics are often used in combination with loop diuretics for a synergistic effect.

62
Q

Furosemide

A

A loop diuretic that works by inhibiting Na-K-2Cl symporters in the ascending limb of the loop of henle effectively blocking Na and Cl transport resulting in increased Na, Cl, and fluid excretion. They are the most potent class of diuretics and are used for treating pulmonary and fluid retention in heart failure patients.

63
Q

Triamterene

A

Potassium sparing diuretic that works by blocking Na channels in the distal tubule and collecting duct. This results in increased Na and fluid excretion. It is a mild diuretic.

64
Q

Mannitol

A

Osmotic diuretic that works by increasing plasma and tubular osmolality, resulting in increased Na and fluid excretion.

65
Q

Acetazolamide

A

Diuretic that works by inhibiting the enzyme carbonic anhydrase.

66
Q

Canagliflozin/Dapagliflozin

A

New oral anti diabetic agent called sodium glucose cotransporter 2 (SGLT2) inhibitors. SGLT2 is a low affinity high capacity transport protein that is responsible for resorbing 90% of filtered glucose in the proximal tubule. SGLT2 inhibition leads to significant urinary glucose loss. They are 2nd or 3rd line anti diabetic drugs that are added to existing oral anti diabetic medications as an alternative to insulin therapy in patients with type 2 diabetes mellitus who fail to achieve their glycemic goals. Side effects include urinary tract and genital mycotic infections due to glycosuria. Increased osmotic diuresis can also cause symptomatic hypotension in some patients (particularly the elderly and those on diuretics). SGLT2 inhibitors should be avoided in patients with moderate to severe renal impairment due to lack of efficacy and increased risk of side effects. For this reason renal function should be assessed before initiating SGLT2 inhibitor therapy and periodically thereafter.

67
Q

Levodopa and Carbidopa

A

Used for parkinson’s disease. Adding carbidopa inhibits the peripheral conversion of levodopa, making more of it available to the brain.) High dose combination levodopa/carbidopa can cause various behavioral changes such as anxiety, agitation, insomnia, confusion, delusions, and hallucinations. Reducing the dose is helpful in alleviating these adverse effects. If reduced dose is not possible then atypical antipsychotics such as clozapine may be helpful.

68
Q

Colchicine

A

Reduces the acute inflammation of gouty arthritis by inhibiting neutrophil migration into the inflamed areas.

69
Q

Allopurinol

A

An isomer of hypoxanthine that lowers serum uric acid levels. It is prescribed to prevent attacks of acute gouty arthritis but is not useful in the treatment of acute flares.

70
Q

Rosuvastatin, Atorvastatin, Simvastatin

A

Statin drugs, Inhibits HMG-CoA reductase (rate limiting step of cholesterol synthesis) leads to high decrease in LDL, a decrease in Triglycerides, and an increase in HDL. Side effects include hepatotoxicity and muscle toxicity.

71
Q

Gemfibrozil, Fenofibrate

A

Fibrates, activate PPAR-alpha, lead to decrease in LDLs, a high decrease in TAGs, and an increase in HDL. Side effects include muscle toxicity (especially when combined with statins) and gallstones.

72
Q

Cholestyramine, Colestipol, Colesevelam

A

Bile acid sequestrants, bind bile acids in the intestine, preventing reabsorption. Decrease LDL. Side effect include Nausea, bloating, cramping, impaired drug and fat soluble vitamin absorption.

73
Q

Niacin

A

Decreases fatty acid release, decreases VLDL synthesis, and HDL clearance. Leading to major increase in HDL, decrease in TAGs and a decrease in LDL. Side effects include flushing and pruritus and hepatotoxicity

74
Q

Ezetimibe

A

Works by decreasing intestinal cholesterol absorption, leading to decreased LDL. Side effects include increased hepatotoxicity when given with statins.

75
Q

Omega 3 fatty acids

A

Decreases synthesis of TAGs. Side effects include nausea.

76
Q

Cocaine

A

Acts as an indirect sympathomimetic by inhibiting the presynaptic reuptake of NE, dopamine, and serotonin. Results in sympathetic stimulation (hypertension, tachycardia, mydriasis) and CNS activation (eg. increased arousal, agitation, seizures). It is also a potent vasoconstrictor that can promote myocardial ischemia by causing coronary artery vasospasm and increased platelet aggregation (thrombus formation). When used intranasally, its vasoconstrictive effects cause local ischemia resulting in mucosal atrophy and nasal septal perforation.

77
Q

Acarbose

A

inhibits alpha-glucosidase in the intestinal brush border, impairing the hydrolysis of polymeric carbohydrates and leading to decreased postprandial glucose absorption. It may indirectly decrease endogenous insulin (and C-peptide) secretion by reducing postprandial hyperglycemia.

78
Q

Sulfonylureas (Glyburide)

A

Increase the insulin secretion rate of residual pancreatic islet beta cells and reduce blood glucose levels in patients with type 2 diabetes mellitus. As a result circulating C peptide levels rise with sulfonylurea use.

79
Q

Modafinil

A

Psychostimulant promotes wakefulness. A non amphetamine stimulant has become the first line agent for narcolepsy because it is effective, well tolerated, and drug abuse is rare. Its mechanism of action is not well described, but it is thought to enhance dopaminergic signaling. Amphetamines are second line agents due to their sympathomimetic side effects (HTN, arrhythmia, psychosis) and risk for dependency.

80
Q

Zolpidem

A

A non benzodiazepine hypnotic used for insomnia.

81
Q

Melatonin

A

Used for treating jet lag and age related insomnia.

82
Q

Ondansetron, Granisetron, Dolasetron

A

5HT-3 receptor antagonists. Highly effective in preventing chemotherapy induced vomiting. These act by blocking vagus mediated nausea and vomiting and blocking serotonin in the chemoreceptor trigger zone. 5HT-3 receptors are located peripherally in the presynaptic nerve terminals of the vagus nerve in the GI tract. These receptors are also present centrally in the chemoreceptor trigger zone and the solitary nucleus and tract.

83
Q

N-acetylcysteine

A

Indicated in acetaminophen overdose, as a mucolytic agent (in patients with influenza, bronchitis, and cystic fibrosis) and as a reno protective agent in certain patients who require IV contrast CT scan, NAC prevents radio contrast induced nephrotoxicity.

84
Q

Leucovorin

A

AKA folinic acid is used in the treatment of methotrexate overdose.

85
Q

Filgrastim

A

Granulocyte colony stimulating factor (GCS-F) analog used to stimulate the proliferation and differentiation of granulocytes. Approved for minimization of granculocytopenia after myelosuppressive chemotherapy.

86
Q

Dexrazoxane

A

Iron chelating agent that can help prevent anthracycline induced (i.e. doxorubicin) cardiotoxicity.

87
Q

Amifostine

A

Cytoprotective free radical scavenger agent used to decrease the cumulative nephrotoxicity associated with platinum containing and alkylating chemotherapeutic agents.

88
Q

Heparin

A

Functions as an anticoagulant by binding and activating antithrombin 3. It has been shown to reduce morbidity and mortality in acute coronary syndrome patients, but it is not an anti platelet agent. Outpatient use is impractical because it must be administered parenterally

89
Q

Streptokinase

A

Thrombolytic agent used in the acute management of thromboembolic events like cerebrovascular accidents and myocardial infarctions where emergent restoration of blood flow is essential.

90
Q

Vitamin K

A

Used to reverse the effects of warfarin, but has no anti coagulant or anti platelet effects.

91
Q

Paclitaxel

A

Cytotoxic chemotherapeutic agent that binds beta tubulin and enhances microtubule polymerization, producing a disorganized array of microtubules within the cell during metaphase and ultimately cell death.

92
Q

Pyrazinamide

A

Works best at relatively acidic pH, as within phagolysosomes. It is most bactericidal to TB organisms engulfed by macrophages. Other first line agents for TB, namely isoniazid, rifampin, and ethambutol have better activity against extracellular TB.

93
Q

Isoniazid

A

Inhibits synthesis of my colic acid, an important constituent of mycobacterial cell wall.

94
Q

Ethambutol

A

Inhibits mycobacterial cell wall synthesis by blocking arabinosyl transferase.

95
Q

Rifampin

A

Inhibits a mycobacterial DNA dependent RNA polymerase

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