Fun 2 Flashcards
Pilocarpine
Muscarinic agonist
Rx. glaucoma and dry mouth
Tertiary amine
Can treat Sjorgen’s syndrome CF test (acts as diaphoretic)
Bethanechol
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
Atropine
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)
Tropicamide
Anti-muscarinic
Rx. Induce mydriasis
Shorter half-life than atropine
Danger of precipitating an attack of narrow-angle glaucoma
Tolterodine
Anti-muscarinic
M3 specific
Rx. incontinence in elderly
Tiotropium
Anti-muscarininc
Quaternary amine
Rx. Inhalation for selectivity (treat COPD/asthma with adrenergic agonist)
Edrophonium
Competitive AChE inhibitor
Rx. Test for MG
Short acting
Quaternary amine
Donepezil
Competitive AChE inhibitor
Tertiary amine
Rx. Early stage Alzheimer treatment
Physostigmine
Carbamoylating AChE inhibitor
Rx. acute glaucoma, atropine poisoning
Tertiary amine
Neostigmine
Carbamoylating AChE inhibitor, Quaternary amine
Rx. paralytic ileus (not chronic), bladder atony
Historical treatment for myasthenia gravis (pyridostigmine used now)
Sarin
Irreversible AChE inhibitor (phosphorylation)
Pralidoxime
AChE reactivator
Rx. Only effective against phosphorylating agents i.e. DFP and sarin
Must be used early - aging enzyme prevents action
Nicotine
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)
Trimethaphan
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)
Succinylcholine
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
d-tubocurarine
NMJ competitive inhibitor
Rx. flaccid paralysis
Vecuronium
NMJ competitive inhibitor
Rx. flaccid paralysis
Adjunct to anasthesia;orthopedic procedures
Antagonized by AChE inhibitors
Botulinum toxin
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
Phenylephrine
a1 agonist
Rx. Limit anesthetic spread, Nasal decongestant, Retinal examination (induce mydriasis; treat hyperemia), Shock
Vasopressor with bradycardia reflex
Brimonidine
a2 agonist
Rx. Eye drops - open angle glaucoma and ocular hypertension
Rx. Gel - rosacea Can increase uveoscleral outflow with prolonged use (PG release)
Clonidine
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
Dobutamine
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)
Albuterol
B2 agonist
Rx. asthma, Short-acting
Terbutaline
B2 agonist
Rx. asthma, Short-acting
Salmeterol
B2 agonist
Rx. asthma, Long acting
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
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
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)
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
Norepinephrine
a1, a2, B1 agonist
Rx. shock
Increased BP (a1)
No baroreceptor decrease in HR (B1 action)
care for other drug effects
Tyramine
Indirect sympathomimetic
Food, not drug
Interaction with MAOIs-Tyramine not metaboilzed, potentiates NE release, HTN, MI-Stroke
Treat with a1-antagonist
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
Ephedrine
Adrenergic agonist and indirect action
Rx narcolepsy; pressor
Orally active
PED
Formerly used for asthma and CNS stimulation (treat narcolepsy)
Methylphenidate
Indirect sympathomimetic
Rx ADHD
CNS stimulant
Individualized dosing
Can cause insomina, anorexia and weight loss
Guanethidine
Adrenergic neuron blocker
Rx. HTN
False NT
Binds to storage vesicle, preventing NE release
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
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
Metyrosine
Blocks tyrosine hydroxylase
Rx. management of pheochromocytoma
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)
Cocaine
Inhibits NE reuptake
Also blocks indirect acting agents
Short term - enhances NE effects (no reuptake)
Long term - blunts NE effects (no vesicle recharge)
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
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
Tamsulosin
a1A-blocker
Rx benign prostatic hypertrophy
Specific to bladder smooth muscle
NOT used for hypertension
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
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
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
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
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
Co-trimoxazole
Sulfamethoxazole and trimethoprim (DHFR inhibitor)
Similar pharmacokinetics
Separately bacteriostatic; bacteriocidal combo (synergistic)
Treat UTIs, respiratory infections, ear/sinus infections and Salmonella/Shigella
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
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
Nitrofurantoin
Damages DNA
Chronic suppression of bacterial UTIs
Rifampin
Allosteric inhibition of DNA-directed RNA Pol.
Broad spectrum - Treat TB; meningococcal
prophylaxis
Resistance common - use in combos
Rifabutin
Allosteric inhibition of DNA-directed RNA Pol.
Treat Mycobacterium avium complex (macrolides first line)
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
Pen G Benzathine
Depot form of Pen G (longer half life)
Oxacillin
Anti-staph penicillin
Acid-stable
Nafcillin
Anti-staph penicillin
Acid-labile
“Big gun”
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
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
Ticarcillin
Anti-pseudomonal penicillin
Active against Gram - rods
Expensive; prominent side effects
Used with clavulonate
Piperacillin
Extended spectrum penicillin
Most active penicillin
Cefazolin
First gen cephalosporin
Active against Gram + and some - rods
Resistant to staph beta-lactamase
Parenteral
Cephalexin
First gen cephalosporin
Active against Gram + and some - rods
Resistant to staph beta-lactamase
Oral
Cefuroxime
Second gen cephalosporin
Increased Gram - coverage
Crosses blood-brain-barrier
Cefoxitin
Second gen cephalosporin
Increased Gram - coverage
Active against anaerobes
Cefotaxime
Third gen cephalosporin
Beta-lactamase resistant
Crosses blood-brain-barrier
Ceftriaxone
Third gen cephalosporin
Longest half-life
First line for gonorrhea
Treat meningitis and Lyme disease
Ceftazidime
Third gen cephalosporin
Anti-pseudomonal
Cefepime
Fourth generation cephalosporin
Most resistant to beta-lacamase
CNS penetration
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
Clavulanic acid
Beta-lactamase inhibitor
No intrinsic anti-bacterial activity
Combined with amoxicillin and ticarcilin
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
Streptomycin
Aminoglycoside
Treat TB, and minor use for tularemia and plague
Combined with penicillin for endocarditis (enterococci or viridans)
Limited use because of resistance
Gentamicin
“Mainline” aminoglycoside
Treat Gram - rods
Resistance common, especially nosocomial
Intrathecal admin for meningitis
Tobramycin
“Mainline” aminoglycoside
Treat Gram - rods
Resistance common, especially nosocomial
Intrathecal admin for meningitis
Amikacin
Aminoglycoside
For gentamicin/tobramycin resistant strains
Resistant to transferase enzymes
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
