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Fun 2 Flashcards

0
Q

Pilocarpine

A

Muscarinic agonist

Rx. glaucoma and dry mouth

Tertiary amine

Can treat Sjorgen’s syndrome CF test (acts as diaphoretic)

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1
Q

Bethanechol

A

Muscarinic agonist (choline ester)

Rx. urinary retention and GI stasis

Resistant to ChE hydrolysis

Must be oral or subQ

Contraindication: asthma, coronary insufficiency, peptic ulcer, or GI obstruction

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2
Q

Atropine

A

Anti-muscarinic prototype

Rx. Blocks PS tone, treat ChE poisoning

Highly selective - competitive inhibitor

Tertiary amine

Intoxication - red, dry, hot, blind, mad and full (treat with physostigmine)

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3
Q

Tropicamide

A

Anti-muscarinic

Rx. Induce mydriasis

Shorter half-life than atropine

Danger of precipitating an attack of narrow-angle glaucoma

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4
Q

Tolterodine

A

Anti-muscarinic

M3 specific

Rx. incontinence in elderly

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5
Q

Tiotropium

A

Anti-muscarininc

Quaternary amine

Rx. Inhalation for selectivity (treat COPD/asthma with adrenergic agonist)

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6
Q

Edrophonium

A

Competitive AChE inhibitor

Rx. Test for MG

Short acting

Quaternary amine

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7
Q

Donepezil

A

Competitive AChE inhibitor

Tertiary amine

Rx. Early stage Alzheimer treatment

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8
Q

Physostigmine

A

Carbamoylating AChE inhibitor

Rx. acute glaucoma, atropine poisoning

Tertiary amine

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9
Q

Neostigmine

A

Carbamoylating AChE inhibitor, Quaternary amine

Rx. paralytic ileus (not chronic), bladder atony

Historical treatment for myasthenia gravis (pyridostigmine used now)

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10
Q

Sarin

A

Irreversible AChE inhibitor (phosphorylation)

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11
Q

Pralidoxime

A

AChE reactivator

Rx. Only effective against phosphorylating agents i.e. DFP and sarin

Must be used early - aging enzyme prevents action

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12
Q

Nicotine

A

Stimulates nicotinic ganglionic receptors (NMJ at high concentrations)

Increases sympathetic and parasympathetic tone and receptors in CNS

Low dose stimulates many organs especially respiratory

Repeated usage dissipates most effects except cardiovascular (high HR and BP)

High dose stimulates and then blocks NMJ –> paralysis

Deters smoking (gives dopamine reward without harmful effects)

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13
Q

Trimethaphan

A

Ganglionic nicotinic receptor antagonist

Rx. hypertensive crisis, controlled hypotension in surgery, nlock autonomic hyperreflexia

Quaternary sulfonium

Blocks autonomic tone (symp > vessels; PS > heart, GI, iris)

Not used often clinically (lots of side effects)

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14
Q

Succinylcholine

A

NMJ blocker - Depolarizing agent/Methonium Initially stimulates NMJ then blocks;

Phase 1 - prolonged depolarization (rapid recovery possible)

Phase 2 - desensitization (slow recovery)

Fast action

Rapidly hydrolyzed by BChE

ChE inhibitors initially potentiate effect

Genetic deficiency in plasma ChE prevents metabolism

Malignant hyperthermia

Electrolyte imbalance from soft tissue damage

Smaller block needed for muscular disorders i.e. myasthenia gravis

OD –> prolonged apnea, CV collapse and histamine release

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15
Q

d-tubocurarine

A

NMJ competitive inhibitor

Rx. flaccid paralysis

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16
Q

Vecuronium

A

NMJ competitive inhibitor

Rx. flaccid paralysis

Adjunct to anasthesia;orthopedic procedures

Antagonized by AChE inhibitors

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17
Q

Botulinum toxin

A

ACh release inhibitor

Rx strabismus, focal dystonia, hyperhidrosis and cosmetics

Cleaves proteins required for synaptic vesicle release

Selective action at NMJ - results in flaccid paralysis

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18
Q

Phenylephrine

A

a1 agonist

Rx. Limit anesthetic spread, Nasal decongestant, Retinal examination (induce mydriasis; treat hyperemia), Shock

Vasopressor with bradycardia reflex

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19
Q

Brimonidine

A

a2 agonist

Rx. Eye drops - open angle glaucoma and ocular hypertension

Rx. Gel - rosacea Can increase uveoscleral outflow with prolonged use (PG release)

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20
Q

Clonidine

A

a2 agonist

Rx. Potentiates anesthesia, treat hot flashes, test for pheochromocytoma

IV admin lowers BP (acts on a2 receptors in lower brainstem limiting symp. outflow)

Side effects: dry mouth, bradycardia and withdrawal symptoms

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21
Q

Dobutamine

A

B1 agonist

Rx. IV infusion for acute, but reversible heart failure (increases CO)

Short half-life (2 min)

C/I for patients with MI (increases O2 demand)

Side effects = angina, HTN, arrythmia, and tachycardia (high doses has a1 effects)

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22
Q

Albuterol

A

B2 agonist

Rx. asthma, Short-acting

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23
Q

Terbutaline

A

B2 agonist

Rx. asthma, Short-acting

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24
Salmeterol
B2 agonist Rx. asthma, Long acting
25
Dopamine
Rx. Used when renal perfusion compromised i.e. shock D1 at low concentration - renal vasodilation B1 at higher concentration - heart a1 at excess concentration - vasopressor
26
Ritodrine
B2 agonist Rx. Relax uterine smooth muscle - arrest preterm labor IV Can cause metabolic and CV effects (tach, dec PVR) tremors, appetite suppression and wakefulness
27
Isoproterenol
B1 and B2 agonist Rx. Increased inotropy and chronotropy Vasodilation at skeletal muscle, mesenteric and renal beds C/I for patients with MI (can cause arrythmia)
28
Epinephrine
a and B agonist, low dose: B1, B2 vs. High dose: a1, B1 Rx. Treat anaphylaxis (a reduces edema; B2 bronchodilates) Rx cardiac arrest, anesthesia, hemostasis
29
Norepinephrine
a1, a2, B1 agonist Rx. shock Increased BP (a1) No baroreceptor decrease in HR (B1 action) care for other drug effects
30
Tyramine
Indirect sympathomimetic Food, not drug Interaction with MAOIs-Tyramine not metaboilzed, potentiates NE release, HTN, MI-Stroke Treat with a1-antagonist
31
Amphetamine
Indirect sympathomimetic Rx narcolepsy and ADHD- powerful stimulant Lipophilic and metabolically blocked (long acting with prominent CNS effects) Orally active Increases BP with bradycardia reflex (can cause arrythmia) Adderall Fatal OD Appetite suppressant (killer combo with thyroid hormone) Tolerance develops quickly
32
Ephedrine
Adrenergic agonist and indirect action Rx narcolepsy; pressor Orally active PED Formerly used for asthma and CNS stimulation (treat narcolepsy)
33
Methylphenidate
Indirect sympathomimetic Rx ADHD CNS stimulant Individualized dosing Can cause insomina, anorexia and weight loss
34
Guanethidine
Adrenergic neuron blocker Rx. HTN False NT Binds to storage vesicle, preventing NE release
35
Methyldopa
Adrenergic neuron inhibitor Rx. HTN Prodrug - metabolite = alpha-methylNE False NT (displaces NE) a2 agonist like clonidine: lower PVR, lower CO = lower BP Adverse effects: sedation, dry mouth, nasal stuffiness, depression and hepatic toxicity
36
Reserpine
Adrenergic neuron blocker Rx HTN, give with diuretic Binds and inactivates neuronal storage vesicles (blocks storage and transport) Depletes catecholamines and serotonin Reduces CO and PVR Causes sedation and psychotic depression
37
Metyrosine
Blocks tyrosine hydroxylase Rx. management of pheochromocytoma
38
Tricyclic Antidepressants
Inhibits NE reuptake Also blocks indirect acting agents Short term - enhances NE effects (no reuptake) Long term - blunts NE effects (no vesicle recharge)
39
Cocaine
Inhibits NE reuptake Also blocks indirect acting agents Short term - enhances NE effects (no reuptake) Long term - blunts NE effects (no vesicle recharge)
40
Phenoxybenzamine
Irreversible, a1 + a2 antagonist Rx. pheochromocytoma Slow acting but long lasting Also inhibits catecholamine uptake transporter Can cause postural hypotension, fluid retention and inability to ejaculate
41
Prazosin
a1 blocker Rx. primary systemic hypertension (with beta blocker or diuretic), short term benefits for CHF Decreases blood pressure Less prominent tachycardia response than nonselective a-blocker Short half-life (compliance issues) Can cause hypotension and fluid retention Favorable lipid proflie
42
Tamsulosin
a1A-blocker Rx benign prostatic hypertrophy Specific to bladder smooth muscle NOT used for hypertension
43
Propanolol
Beta-blocker Lipophilic High dosage allows 1x daily admin. Sustained release prep available (10) Rx. HTN, angina, HF, acute panic syndrome, pheochromocytoma, hyperthyroidism, hypertrophic obstructive cardiomyopathy, acute dissecting aortic aneurysm, open angle glaucoma, prophylaxis for migraine
44
Carvedilol
Beta-blocker and a1-blocker (two isoforms metabolized at different rates) Antioxidant??? Interest in CHF treatment (10) Rx. HTN, angina, HF, acute panic syndrome, pheochromocytoma, hyperthyroidism, hypertrophic obstructive cardiomyopathy, acute dissecting aortic aneurysm, open angle glaucoma, prophylaxis for migraine
45
Metoprolol
B1-blocker Short half-life Extended-release prep available Genetic differences in metabolism (10) Rx. HTN, angina, HF, acute panic syndrome, pheochromocytoma, hyperthyroidism, hypertrophic obstructive cardiomyopathy, acute dissecting aortic aneurysm, open angle glaucoma, prophylaxis for migraine
46
Atenolol
B1-blocker Longer half-life than metoprolol Limited CNS penetrance (10) Rx. HTN, angina, HF, acute panic syndrome, pheochromocytoma, hyperthyroidism, hypertrophic obstructive cardiomyopathy, acute dissecting aortic aneurysm, open angle glaucoma, prophylaxis for migraine
47
Sulfisoxazole
Competitive inhibitor of DAS; Pseudosubstrate Treat Nocardia and minor UTIs Bacteriostatic Resistance due to increase pABA production or altered DAS Good GI absorption. Distributes to CSF Antagonized by tissue breakdown products Toxicity: Allergies, GI, hemolysis w/out G6PDH, crystalluria
48
Co-trimoxazole
Sulfamethoxazole and trimethoprim (DHFR inhibitor) Similar pharmacokinetics Separately bacteriostatic; bacteriocidal combo (synergistic) Treat UTIs, respiratory infections, ear/sinus infections and Salmonella/Shigella
49
Ciprofloxacin
Fluoroquinolone Does not have strong activity against Gram + Aerobes only Inhibit DNA topoisomerase-gyrase complex Oral; No CSF distribution Avoid cations i.e. milk, antacids, vitamins Inhibits cartilage formation - avoid with children and pregnancy
50
Levofloxacin
Fluoroquinolone More Gram (+) activity i.e. strep Inhibit DNA topoisomerase-gyrase complex Oral; No CSF distribution Avoid cations i.e. milk, antacids, vitamins Inhibits cartilage formation - avoid with children and pregnancy
51
Nitrofurantoin
Damages DNA Chronic suppression of bacterial UTIs
52
Rifampin
Allosteric inhibition of DNA-directed RNA Pol. Broad spectrum - Treat TB; meningococcal prophylaxis Resistance common - use in combos
53
Rifabutin
Allosteric inhibition of DNA-directed RNA Pol. Treat Mycobacterium avium complex (macrolides first line)
54
Penicillin G
Narrow spectrum penicilin Acid-labile; short half life Active against Gram + (not enterococcus), Gram - cocci (gonnorhea resistant) and syphilis Probenecid blocks removal into urine
55
Pen G Benzathine
Depot form of Pen G (longer half life)
56
Oxacillin
Anti-staph penicillin Acid-stable
57
Nafcillin
Anti-staph penicillin Acid-labile "Big gun"
58
Ampicillin
Broad spectrum penicillin Active against some Gram - rods Treat URIs and UTIS; meningitis and salmonella occasionally Acid stable; sensitive to beta-lactamases Not as active against Gram + as Pen G
59
Amoxicillin
Broad spectrum penicillin Better F than ampicillin Active against some Gram - rods Treat URIs and UTIS; meningitis and salmonella occasionally Acid stable; sensitive to beta-lactamases Not as active against Gram + as Pen G
60
Ticarcillin
Anti-pseudomonal penicillin Active against Gram - rods Expensive; prominent side effects Used with clavulonate
61
Piperacillin
Extended spectrum penicillin Most active penicillin
62
Cefazolin
First gen cephalosporin Active against Gram + and some - rods Resistant to staph beta-lactamase Parenteral
63
Cephalexin
First gen cephalosporin Active against Gram + and some - rods Resistant to staph beta-lactamase Oral
64
Cefuroxime
Second gen cephalosporin Increased Gram - coverage Crosses blood-brain-barrier
65
Cefoxitin
Second gen cephalosporin Increased Gram - coverage Active against anaerobes
66
Cefotaxime
Third gen cephalosporin Beta-lactamase resistant Crosses blood-brain-barrier
67
Ceftriaxone
Third gen cephalosporin Longest half-life First line for gonorrhea Treat meningitis and Lyme disease
68
Ceftazidime
Third gen cephalosporin Anti-pseudomonal
69
Cefepime
Fourth generation cephalosporin Most resistant to beta-lacamase CNS penetration
70
Imipenem
Carbopenem Active against anaerobes Resistant to beta-lactamases Broad spectrum; "last resort" Inactivated by renal dipeptidase (given with cilistatin) Carbopenem resistant enterococcus emerging issue
71
Clavulanic acid
Beta-lactamase inhibitor No intrinsic anti-bacterial activity Combined with amoxicillin and ticarcilin
72
Vancomycin
Glycopeptide Sequesters D-ala-D-ala from transpeptidase Treat MRSA, C. difficile and viridans Ototoxicity and nephrotoxicity CSF penetration Resistance from D-ala-D-lac
73
Streptomycin
Aminoglycoside Treat TB, and minor use for tularemia and plague Combined with penicillin for endocarditis (enterococci or viridans) Limited use because of resistance
74
Gentamicin
"Mainline" aminoglycoside Treat Gram - rods Resistance common, especially nosocomial Intrathecal admin for meningitis
75
Tobramycin
"Mainline" aminoglycoside Treat Gram - rods Resistance common, especially nosocomial Intrathecal admin for meningitis
76
Amikacin
Aminoglycoside For gentamicin/tobramycin resistant strains Resistant to transferase enzymes
77
Tetracycline
Tetracycline Binds 30S - prevents tRNA access to A site (bacteriostatic) Treat Rickettsia, mycoplasma and chlamydia Resistance from efflux pump Don't ingest with cations Lowest F and shortest half-life Renal excretion Toxicity: superinfection, hepatoxicity, phototoxicity and calcified tissue

Pharm (6 decks)

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