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Pharm > Fun 2 > Flashcards

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
Q

Salmeterol

A

B2 agonist

Rx. asthma, Long acting

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25
Q

Dopamine

A

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

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26
Q

Ritodrine

A

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

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27
Q

Isoproterenol

A

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)

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28
Q

Epinephrine

A

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

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29
Q

Norepinephrine

A

a1, a2, B1 agonist

Rx. shock

Increased BP (a1)

No baroreceptor decrease in HR (B1 action)

care for other drug effects

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30
Q

Tyramine

A

Indirect sympathomimetic

Food, not drug

Interaction with MAOIs-Tyramine not metaboilzed, potentiates NE release, HTN, MI-Stroke

Treat with a1-antagonist

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31
Q

Amphetamine

A

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
Q

Ephedrine

A

Adrenergic agonist and indirect action

Rx narcolepsy; pressor

Orally active

PED

Formerly used for asthma and CNS stimulation (treat narcolepsy)

33
Q

Methylphenidate

A

Indirect sympathomimetic

Rx ADHD

CNS stimulant

Individualized dosing

Can cause insomina, anorexia and weight loss

34
Q

Guanethidine

A

Adrenergic neuron blocker

Rx. HTN

False NT

Binds to storage vesicle, preventing NE release

35
Q

Methyldopa

A

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
Q

Reserpine

A

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
Q

Metyrosine

A

Blocks tyrosine hydroxylase

Rx. management of pheochromocytoma

38
Q

Tricyclic Antidepressants

A

Inhibits NE reuptake

Also blocks indirect acting agents

Short term - enhances NE effects (no reuptake)

Long term - blunts NE effects (no vesicle recharge)

39
Q

Cocaine

A

Inhibits NE reuptake

Also blocks indirect acting agents

Short term - enhances NE effects (no reuptake)

Long term - blunts NE effects (no vesicle recharge)

40
Q

Phenoxybenzamine

A

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
Q

Prazosin

A

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
Q

Tamsulosin

A

a1A-blocker

Rx benign prostatic hypertrophy

Specific to bladder smooth muscle

NOT used for hypertension

43
Q

Propanolol

A

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
Q

Carvedilol

A

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
Q

Metoprolol

A

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
Q

Atenolol

A

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
Q

Sulfisoxazole

A

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
Q

Co-trimoxazole

A

Sulfamethoxazole and trimethoprim (DHFR inhibitor)

Similar pharmacokinetics

Separately bacteriostatic; bacteriocidal combo (synergistic)

Treat UTIs, respiratory infections, ear/sinus infections and Salmonella/Shigella

49
Q

Ciprofloxacin

A

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
Q

Levofloxacin

A

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
Q

Nitrofurantoin

A

Damages DNA

Chronic suppression of bacterial UTIs

52
Q

Rifampin

A

Allosteric inhibition of DNA-directed RNA Pol.

Broad spectrum - Treat TB; meningococcal
prophylaxis

Resistance common - use in combos

53
Q

Rifabutin

A

Allosteric inhibition of DNA-directed RNA Pol.

Treat Mycobacterium avium complex (macrolides first line)

54
Q

Penicillin G

A

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
Q

Pen G Benzathine

A

Depot form of Pen G (longer half life)

56
Q

Oxacillin

A

Anti-staph penicillin

Acid-stable

57
Q

Nafcillin

A

Anti-staph penicillin

Acid-labile

“Big gun”

58
Q

Ampicillin

A

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
Q

Amoxicillin

A

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
Q

Ticarcillin

A

Anti-pseudomonal penicillin

Active against Gram - rods

Expensive; prominent side effects

Used with clavulonate

61
Q

Piperacillin

A

Extended spectrum penicillin

Most active penicillin

62
Q

Cefazolin

A

First gen cephalosporin

Active against Gram + and some - rods

Resistant to staph beta-lactamase

Parenteral

63
Q

Cephalexin

A

First gen cephalosporin

Active against Gram + and some - rods

Resistant to staph beta-lactamase

Oral

64
Q

Cefuroxime

A

Second gen cephalosporin

Increased Gram - coverage

Crosses blood-brain-barrier

65
Q

Cefoxitin

A

Second gen cephalosporin

Increased Gram - coverage

Active against anaerobes

66
Q

Cefotaxime

A

Third gen cephalosporin

Beta-lactamase resistant

Crosses blood-brain-barrier

67
Q

Ceftriaxone

A

Third gen cephalosporin

Longest half-life

First line for gonorrhea

Treat meningitis and Lyme disease

68
Q

Ceftazidime

A

Third gen cephalosporin

Anti-pseudomonal

69
Q

Cefepime

A

Fourth generation cephalosporin

Most resistant to beta-lacamase

CNS penetration

70
Q

Imipenem

A

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
Q

Clavulanic acid

A

Beta-lactamase inhibitor

No intrinsic anti-bacterial activity

Combined with amoxicillin and ticarcilin

72
Q

Vancomycin

A

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
Q

Streptomycin

A

Aminoglycoside

Treat TB, and minor use for tularemia and plague

Combined with penicillin for endocarditis (enterococci or viridans)

Limited use because of resistance

74
Q

Gentamicin

A

“Mainline” aminoglycoside

Treat Gram - rods

Resistance common, especially nosocomial

Intrathecal admin for meningitis

75
Q

Tobramycin

A

“Mainline” aminoglycoside

Treat Gram - rods

Resistance common, especially nosocomial

Intrathecal admin for meningitis

76
Q

Amikacin

A

Aminoglycoside

For gentamicin/tobramycin resistant strains

Resistant to transferase enzymes

77
Q

Tetracycline

A

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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