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Autonomics, Cardiac, Anti-coag
1. MoA 2. Use 3. Side Effects, 4. Interactions
106
Pharmacology
Professional
01/19/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Sildenafil
Definition
(aka Viagra)
1. phosphodiesterase type 5, inhibitor
enhance effect of N.O.
2. ED; also FDA for Pulm HTN!
3. a phosphoDE type 6 in eye has some reactivity to drug = potential vision alteration!
Term
tamsulosin (FLOMAX)
Definition
1. alpha1 antagonist, more selective to urinary flow
2. urinary retention, BPH
Term
metyrosine
Definition
1. competitive inhibitor of tyrosine hydroxylase (tyrosine to DOPA)
2. pheochromocytoma
3. Sedation/depression, crystalluria, GI upset
Term
methyldopa
Definition

1. centrally acting α2 agonist; Also aids platlet aggregation and decr insulin secretion

2. HTN in pregnancy & RENAL Dz

(3. Hepatotoxicity, hemolytic anemia)

Term
reserpine
Definition
1. irriversibly blocks VMAT /depletes endogenous catecholamine
2. HTN (rarely nowadays)
3. SEVERE DEPRESSION, CNS effects, sedation. DONT give to suicidal pts
Term
Guanethidine
Definition
1. Uncoupler of Stim/Secretion: uptaken by NET thus blocking it, displaces and slowly depletes endogenous NE, inhibits vesicular fusion with membrane
2.HTN - no longer used
Term
cocaine
Definition
1. inhibition of NET (uptake 1) & Na-Ch blocker
2. surgical topical anesthetic for nasal muscosa or lacrimal ducts
3. Sympathetic hyperactivity
Term
Amphetamine
Definition

1. potent indirect sympathomimetic, releases stored catecholamines

2. Narcolepsy, ADHD, appetite suppressant & weight loss, alertness, mood

3. depression, palpitation, vasomotor disturbance, agitation, confusion; rapid tolerance; ARRHYTHMIA, ANGINA, STROKE...

Term
Methamphetamine
Definition
1. potent indirect sympathomimetic of especially CNS
2. appetite suppressant
3. similar adverse effects as ephedrine
Term
Ephedrine
Definition

1.  indirect general sympathomimetic, releases stored catecholamines

2. decongestant, urinary incontinence, hypotension

3. ↑BP and stroke; arrythmias, MI, CNS stim, seizures

4. Do NOT take with MAOI

Term
Pseudoephedrine (SUDAFED)
Definition
1. mostly indirect sympathomimetic to alpha receptors(some direct alpha and beta stimulation, some CNS effects)

2. decongestant, weight loss, appetite suppressant

3. ↑BP and stroke; arrythmias, MI, CNS stim, seizures

4. Do NOT take with MAOI
Term
Methylphenidate (RITALIN)
Definition
1. ephedrine-like indirect sympathomimetic, CNS stimulant; displaces NE from vesicle
2. ADHD
3. Unclear
Term
Tyramine
Definition
1. indirect sympathomimetic; metabolized in GI/liver by MAO, with MAOI accumulates in vesicles, changed to octopamine and stored
3. wine and cheese syndrome (hypertensive crisis)
Term
entacapone
Definition
1. COMT inhibitor
2. adjunct therapy for Parkinsons
Term
iproniazid;
(also tranylcypromine, phenelzine)
Definition
1. MAO inhibitor
2. an antidepressant
Term
metaproterenol, albuterol, salmeterol
Definition

1. selective β2 agonists

2. Asthma; albuterol & metaproterenol for acute attacks; salmeterol for long-term tx

3. excessive cardiac stim, tremor

Term
clonidine
Definition

1. α2 receptor agonist in CNS; get ↓SNS to HR and vessels; Also aids platlet aggregation and ↓ insulin secretion

2. HTN in pregnancy & RENAL Dz

(3. dry mouth, sedation; WITHDRAWL)

Term
dobutamine
Definition

1. β1 receptor agonist, some β2 = more INOTROPIC

2. cardiac failure, Cardiac stress test!

 

Term
terbutaline
Definition

1. β2 agonist

2. premature labor, to reduce uterine cntrx

3. tachycardia

Term
dopamine
Definition

1. Agonist at D1/D2 kidney receptors >  α/β receptors

2. SHOCK to ↑renal perfusion, some CHF

 

Term
epinephrine
Definition

1. agonist (non-selective) to all alpha and beta receptors 2. anaphylaxis or cardiac arrest; glaucoma, asthma, hypotension

3. excessive cardiac stimulation

Term
isoproterenol
Definition

1. stimulates all beta receptors (NOT alpha)

2. AV block (rare)

3. excessive cardiac stimulation

Term
norepinephrine
Definition

1. stimulate alpha and beta-1 receptors (NOT beta2)

2. Shock (but would ↓renal perfusion)

Term
phenylephrine
Definition
1. alpha1-receptor agonist to constrict vascular smooth muscle
2. topically for nasal congestion or opthalmic hyperemia, and shock (IV)
3. bradycardia (the relex ↓HR)
Term
salmeterol
Definition
1. stimulates β2 receptors, longer onset, but longer duration
2. long-term Asthma (but not rescue tx), premature labor
3. excessive cardiac stim, tremor
Term
atenolol
Definition
1. β1 antagonist
2. HTN, angina, arrhythmias, ischemic heart, CHF
3. bronchocontrictions, bradycardia, hypoglycemia
Term
carvedilol
Definition

1. non selective β-blocker; ↓CO/HR = ↓O2 demand

also blocks β at JGA = ↓RAAS

2. HTN, angina, MI to DECR MORTALITY!, CHF

 

Term
esmolol
Definition

1. Ultra Short acting β-blocker

2. limit catecholamine-mediated cardiac stimulation in surgery; SVTs

3. succeptible to enzymatic hydrolysis in blood

Term
labetalol
Definition

1. nonselective β blocker

2. HTN in pregnancy

3. postural hypotension, broncho-constriction

Term
metoprolol
Definition
1. "cardio-selective" β1 blocker
2. HTN, angina, arrhythmias, ischemic heart, CHF (better for asthmatics)
Term
Phenoxybenzamine
Definition
1. irreversible non-selective α-blocker
2. pheochromocytoma
3. excessive cardiac stim
Term
phentolamine
Definition
1. Competitive, non-selective α-blocker
2. pheochromocytoma
3. excessive cardiac stim
Term
pindolol
Definition
1. partial agonist at ALL β receptors
2. HTN, angina, arrhythmias, ischemic heart, CHF
3. bronchocontrictions, bradycardia, hypoglycemia (all to a lesser extent that β-antagonists)
Term
prazosin
Definition
1. α1-competitive antagonist
2. HTN, CHF, BPH
3. "first dose" phenomenon, hypotention and impotence
Term
propranolol
Definition

1. competitive antagonist to all β receptors, membrane stabilizing activity, (and ↓phase 4 depolarization)

2. HTN, angina, arrhythmias, ischemic heart

Prevent sudden death post MI

3. cardiac depression, bronchoconstriction, hypoglycemia, sedation, nightmares, insomnia

Term
terazosin
Definition
1. α1-competitive antagonist
2. HTN, CHF, BPH
3. "first dose" phenomenon, hypotention and impotence
Term
timolol
Definition
1. non-selective β-blocker, decreases aqueous humor production
2. Glaucoma
3. can be absorbed to systemic (heart, airways)
Term
atropine
Definition
1. muscarinic - antagonist;
2. treat muscarinic hyperactivity such as in nerve gas or insecticide poisoning; Parkinson's
3. 1st-dry mouth and kids hyperthermia, then glaucoma worsens, then CV system, then resp & bladder, GI, last CNS
Term
donepezil
Definition
1. cholinesterase (reversible) inhibitor, very lipid soluble = enters CNS
2. Alzheimer's, to delay/tx symptoms
Term
echothiophate
Definition
1. AchE-i; irreversible substrate inhibitor (organophosphate); forms stable essentially irreversible complex
2. historically for glaucoma
Term
edrophonium (TENSILON)
Definition
1. cholinesterase (reversible) inhibitor, occlude active site
2. diagnostic
Term
neostigmine
Definition
1. QUATERNARY cholinesterase carbamate reversible inhibitor, serves as a more stable substrate
2. Mysasthenia Gravis, paralytic ileus, bladder atony
Term
physostigmine
Definition
1. TERTIARY cholinesterase carbamate reversible inhibitor, serves as a more stable substrate (DOES enter CNS)
2. Myasthenia Gravis; Atropine Overdose!
Term
pralidoxime (2-PAM)
Definition
1. a strong neutrophile - REGENERATES AchE; can pull off organophosphates before 'aging' occurs (does NOT enter CNS)
2. antidote to organophosphate intox
Term
malathion/parathion
Definition
insecticides - organophosphate cholinesterase inhibitors;
-depolarizing blockade in nicotinic receptors
-hyperactivity at muscarinic receptors
Term
sarin/VX
Definition
Military Nerve Gas - an organophosphate cholinesterase inhibitor; VERY short aging time
-depolarizing blockade in nicotinic receptors
-hyperactivity at muscarinic receptors
Term
bethanechol
Definition
1. Synthetic ACH analog
2. Ileus, Urinary Retention
Term
methacholine
Definition
1. 1. synthetic Ach analog
2. provocative test for hyperreactive airways
3. cardiovascular & respiratory effects
Term
muscarine
Definition
1. muscarine receptor agonist (cholinomimetic)
Term
nicotine
Definition
1. activates nicotinic receptors (ligand-gated ion channels)
Term
pilocarpine
Definition
(from Jaborandi "what causes slobbering")
1. muscarinic receptors direct Agonist
2. historically, glaucoma; relieve dry mouth, Sjogren's
3. can be absorbed systemically, widespread PSNS and CNS effects
Term
succinylcholine
Definition
1. depolarizing blockade at nicotinic receptors
2. to create paralysis during surgery
3. muscle soreness, hyperkalemia
Term
varenicline
Definition
1. a neuronal nicotinic receptor partial agonist; produces dopamine release in 'reward center', also blocks binding of nicotine
2. smoking cessationg
3. NAUSEA, headache, abnormal dreams
Term
hexamethonium
Definition
1. Ganglionic nicotinic receptor antagonist - Paralysis of ENTIRE autonomic nervous system!
2. (limited use) HTN, dissecting aortic aneurysm, autonomic hyperreflexia, to control hemorrhage
3. "Hexamethonium Man" SNS predominates in BP, PSNS predominates in HR
Term
ipratropium+
Definition
1. antimuscarinic
2. asthma, COPD
3. toxic doses can cause hypotension(ganglion blockade), muscle weakness (NMJ blockade)
Term
scopolamine
Definition
1. anti-muscarinic, esp in CNS
2. motion sickness, via transdermal patch
3. sedation, anterograde anmesia
Term
tolterodine
Definition
1. antimuscarinic with no apparent selectivity
2. OverActive Bladder
3. typical anticholinergic effects, but for some reason at less incidence than other similar drugs
Term
d-tubocurarine
Definition
1. Non-depolarizing, competitive antagonist to NMJ nicotinic receptors
2. induce paralysis for surgery
3. fall in arterial pressure
Term
Quinidine
Definition

Class 1A Fast Na-blocker, with Anti-Muscarinic effects

1. slow conduction, increase AP duration,

and increase effective refractory

3. Torsade de pointes!

 

Term
procainamide/disopyramide
Definition

Class 1A Fast Na-blocker

1. slow conduction, increase AP duration,

and increase effective refractory

(NAPA metabolite has some K-blocking, too)

3. Torsade de pointes!

 

Term
lidocaine/mexiletine/tocainide
(also phenytoin)
Definition
Class 1B quick Fast Na-blocker
1. slows conduction but DECREASES AP duration and effective refractory period
2. Acute ventric. arryth esp post-MI
Term
flecainide/encainide/propafenone
Definition
Class 1C slow Fast Na-blocker
1. slows conduction
*BUT also exhibits some K-blocking aka increases AP duration and refractoriness
2. for V-Tach's that progress to VF; a last resort
3. PROARRYTHMIC! contra post-MI
Term
metoprolol
Definition
B1-blocker
1. B1 seems to mediate myocardial apoptosis; so this blocks that!
2. CHF
Term
amiodarone
Definition

Class 3 K-Channel blocker

1. Prolong AP duration by prolonging refractory period

in myocytes and purkinje fibers

(Actually exhibits class 1-4 characteristics)

3. Pulmonary Fibrosis

Term
diltiazem
Definition

Class 4 voltage gated Ca-Channel blocker

1. major response to slow AP responders (aka SA, AV nodes or damage myocytes)

↓HR and AV conduction

Term
digoxin (LANOXIN)
Definition

1. inhibit Na/K ATPase; vagal stimulation

= increased contractility, yet decr. HR and O2 consumption

2. Heart Failure and AFib

 

Term
adenosine
Definition
ultra short 1/2 life, activates K channels to decrease AV conduction
Term
nitroglycerin
Definition

conversion to NO; vasodilator

1. decrease LVEDP, and afterload

2. ischemic heart

3. orthostatic HTN, reflex tachy, TOLERANCE

Term
isosorbide dinitrate
Definition
organic nitrate; longer acting that NTG
Term
verapamil
Definition

Class 4 voltage gated Ca-Channel blocker

1. major response to slow AP responders

(aka SA, AV nodes or damage myocytes)

↓HR and AV conduction

Also a vasodilator!

Term
nifedipine
Definition

A type 2 (predominantly vascular) Ca-Channel Blocker

minimal effect on AV, SA, or contractility

2. ischemic heart

Term
inamrinone/milrinone
Definition
phosphodiesterase type 3 inhibitor
1. cardiac specific; increase contractility, and vasodilation
2. short term for acute CHF
3. "Killrinone" aka arrhythmogenic
Term
hydralazine (APRESOLINE)
Definition
1. an NO Pro-drug; "nitroglycerin's cousin" dilates mostly ARTERIOLES = decr afterload
2. HTN in pregnancy(+methyldopa a-agonist), CHF, Severe HTN
3. lupus-like syndrm; compensory tachycard.
Term
nitroprusside
Definition
conversion to NO; vasodilator
2. Malignant HTN!
3. CN- toxicity
Term
captopril
Definition

*ACE inhibitor*

1. also can ↑bradykinin release (vasodilate)

2. MANDATORY use in Chronic HF

3. persistant cough from ↑bradykinin,

HYPERKALEMIA, short 1/2 life

Term
enalapril
Definition

*ACE inhibitor*

1. also can ↑bradykinin release (vasodilate)

2. MANDATORY use in Chronic HF

3. persistant cough from ↑bradykinin,

HYPERKALEMIA, longer 1/2 life

Term
lisinopril
Definition

*ACE inhibitor*

1. also can ↑bradykinin release (vasodilate)

2. MANDATORY use in Chronic HF

3. persistant cough from ↑bradykinin,

HYPERKALEMIA (aka arrythmia possible)

Term
valsartan
Definition
Angiotensin 2, AT1-receptor blocker
2. don't ↑bradykinin, thus no cough
3. angioedema
Term
losartan
Definition
Angiotensin 2, AT1-receptor blocker
2. don't ↑bradykinin, thus no cough
3. angioedema
Term
fenoldopam
Definition
1. D1 agonist; Used for vasodilation property
2. HTN, Shock-to incr perfusion to kidneys!
Term
mirtazapine
Definition
1. a2 blocker
2. depression
Term
Heparin
Definition
1. Binds to AntiThrombin3 & accelerates action inactivation of 9, 10, & thrombin
2. current clotting, prophylaxis (DVT, PE, MI, AFib, big procedures
3. bleeding, Hep-induced Thrombocytopenia (IgG), allergic rxn since hep comes from pig and beef mast cells
Term
enoxaparin (LMWH)
Definition
1. binds AT3 for selective-inhibition to factor 10, bc too small to also bind thrombin
2. abdm surg, hip/knee replacement
3. bleeding, thrombocytopenia; but requires less monitoring, greater T.I.
Term
fondaparinux
Definition
1. synthetic, with a much longer 1/2Life than LMWH
2. prevent orthopedic DVTs, tx DVT/PE
3. bleeding, much LESS thrombocytopenia or allergy hazard; Not for renal dysfunction pts
Term
protamine sulfate
Definition
1. a Large cation protein that complexes with Heparin (large anion)
2. to rapidly reverse heparin effects
Term
warfarin
Definition
1. Block VitK Epoxide Reductase to inhibit synthesis of 2,7,9,10; get to INR of 2-3;
2. Prophylaxis/tx DVT, PE, MI, AFib
3. hemorrhage; initial HYPERcoag from knocking out Pro-C 1st; Contra to Pregnancy!
4. ~99% highly bound, uses P450s
Term
Vitamin K
Definition
1. bypasses warfarin's inhibition of VitK epoxide reductase; diminish Warf. effect
Term
lepirudin
Definition
Anti-platlet & Anti-Coag.
1. Directly inhibit thrombin enzyme active site (no co-factor needed) to prevent fibrin activation
2. Hep-induced thrombocytopenia or risk of it, surgery prophylaxis
3. renal excretion so caution to renal dysfx pt
Term
desirudin
Definition
Anti-platlet & Anti-Coag.
1. Directly inhibit thrombin enzyme active site (no co-factor needed) to prevent fibrin activation
2. Hep-induced thrombocytopenia or risk of it, surgery prophylaxis
Term
bivalirudin
Definition
Anti-platlet & Anti-Coag.
1. Directly inhibit thrombin enzyme active site (no co-factor needed) to prevent fibrin activation
2. Hep-induced thrombocytopenia or risk of it, surgery prophylaxis
Term
argatroban
Definition
Orally available Hirudin
1. metabolized in liver so ok for renal dysfx patients
Term
dabigatran
Definition
Orally available Hirudin
1. cleared by renal, so ok for hepatic dysfx patients
2. stroke prevention with AFib
Term
dipyridamole
Definition
1. ↑cAMP that prevents platelet activation; via blocking phosphodiesterase which degrades cAMP and blocking adenosine uptake which would normall ↓cAMP (give w/ ASA)
2. pt with increased stroke risk
3. Headache; contraindications like ASA
Term
eptifibatide
Definition
1. GPIIa/IIIb receptor reversible inhibitor = blocks x-linking and aggregation of platelets
2. Prevent MI
3. Bleeding; Contra to Renal Dysfx pt
Term
abciximab
Definition
1. Mouse-Human Ab to GPIIa/IIIb receptor = blocks x-linking and aggregation of platlets
2. Prevent MI
3. Bleeding
Term
tirofiban
Definition
1. a tyrosine analog that binds and inhibits GPIIa/IIIb receptor = blocks x-linking and aggregation of platelets
2. Prevent MI
3. Bleeding; contra to hepatic dysfx pts
Term
ticlopidine
Definition
1. ADP-Receptor P2Y Inhibitor = ↑cAMP and inhibition of platelet activation
2. prevent MI in failed ASA use
3. Neutropenia/agranulocytosis!; contra to Prior TIA or Stroke, CABG, active bleeding
Term
clopidogrel
Definition
1. ADP-Receptor P2Y Inhibitor = ↑cAMP and inhibition of platelet activation
2. prevent MI in failed ASA use
3. Better tolerated; Neutropenia, agranulocytosis; contra to Prior TIA or Stroke, CABG, active bleeding; metabo by CYP2C19
Term
prasugrel
Definition
1. ADP-Receptor P2Y Inhibitor = ↑cAMP and inhibition of platelet activation; More Potent!
2. prevent MI in failed ASA use
3. BLEEDING; Neutropenia, agranulocytosis; contra to Prior TIA or Stroke, CABG, active bleeding
Term
ticagrelor
Definition
1. ALLOSTERIC ADP-Receptor P2Y reversible Inhibitor = ↑cAMP and inhibition of platelet activation
2. prevent MI in failed ASA use
3. Neutropenia/agranulocytosis; contra to Prior TIA or Stroke, CABG, active bleeding
Term
streptokinase
Definition
1. tPA isolated from Streptococci; activates plasmin
2. MI, acute ischemic stroke or PE
3. massive fibrinolysis
Term
alteplase (r tPA)
Definition
1. recombinant tPA that binds only to fresh thrombi before activating plasmin
2. MI, acute ischemic stroke or PE
3. massive fibrinolysis
Term
aminocaproic acid
Definition
1. lysine analog - plasmin Inhibitor
2. streptokinase/alteplase OD/toxicity
Term
diphenhydramine, dimenhydrinate
chlorpheniramine, promethazine, hydroxyzine
Definition
1. 1st generation H1-Antihistamine (can get to CNS histamine receptor in NST) depress labyrinth excitability; MAJOR AntiMuscarinic!
2. allery; Motion Sickness; early tx of parkinson's symptoms
3. SEDATION, antiMusc. effects
Term
cetirizine
Definition
1. 2nd Gen H1-antihistamine; minimal to no antiMusc effects
2. allergy only
3. FAR less sedation = you're free to "cet and dine" on this drug.
Term
loratadine
fexofenadine
desloratadine
Definition
1. 2nd Gen H1-antihistamine; minimal to no antiMusc effects
2. allergy only
3. FAR less sedation = you're free to "cet and dine" on this drug.
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