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Pharm drugs 2
Drugs in lectures for exam 2
63
Pharmacology
Professional
10/11/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
acetylcholine
Definition

class:  parasympathomimetics

type:  endogenous cholinergic

receptor:  nicotinic, muscarinic

effects:  nonspecific, rarely ophthalmic

clinical use:  nonspecific

Term
Bethanechol
Definition

  • class:  parasympathomimetic
  • type:  direct-acting synthetic choline ester
  • receptor:  muscarinic (M3)
  • specific effects:  detrusor contraction, trigone/sphincter relaxation
  • clinical use:  empty bladder in the absence of obstruction

Term
Muscarine
Definition

  • class:  parasympathomimetic
  • type:  direct-acting cholinomimetic alkaloid
  • receptor:  muscarinic
  • specific effects:  nonspecific
  • not used clinically
  • factor in mushroom toxicity

Term
Pilocarpine
Definition

  • class:  parasympathomimetic
  • type:  direct-acting cholinomimetic alkaloid
  • receptor:  muscarinic
  • specific effects:  topical ophthalmic to induce pupil constriction
  • clinical use:  induce miosis, reduce intraocular pressure in glaucoma, promote salivation

Term
physostigmine
Definition

  • class:  AChE inhibitors
  • type:  reversible covalent inhibitor
  • receptor:  decreases degradation of ACh
  • specific effects:  enters the CNS
  • clinical use:  counter CNS symptoms of anticholinergic intoxication

Term
Neostigmine
Definition

  • class:  AChE inhibitor
  • type:  reversible covalent inhibitor
  • receptor:  acts by decreasing degradation of ACh
  • specific effects:  stimulate visceral smooth muscle

Term

Organophosphates

(Insecticides)

(Nerve Gases)

Definition

  • class:  AChE inhibitor
  • type:  irreversible covalent inhibitors
  • receptor:  inhibits activity of AChE
  • symptoms of toxicity:  SLUDGE, DUMBELS
  • treatment:  cholinesterase "reactivators" (2-PAM)

Term
Atropine
Definition

 

  • class:  anticholinergic
  • type:  natural alkaloid
  • receptor:  competitive inhibition of muscarinics
  • specific effects:  enters CNS, decreases salivary and airway secretions
  • clinical use:  adjunct during anesthesia, relieves AChE inhibitor toxicity
  • NOTE:  rabbits have atropinases

 

Term
Scopolamine
Definition

 

  • class:  anticholinergic
  • type:  natural alkaloid
  • receptor:  competitive inhibition of muscarinics
  • specific effects:  enters CNS
  • clinical use:  low dose causes slight sedation, high dose causes excitement, antiemetic

 

Term
Glycopyrrolate
Definition

  • class:  anticholinergic
  • type:  synthetic alkaloid derivative
  • receptor:  competitive inhibition of muscarinics
  • specific effects:  decrease salivary and airway secretions, decrease bradycardia (does not enter CNS)
  • clinical use:  adjunct during anesthesia

Term
Tropicamide
Definition

  • class:  anticholinergic
  • type:  synthetic alkaloid derivative
  • receptor:  competitive inhibition of muscarinics
  • specific effects:  ophthalmic topical produces mydriasis and cycloplegia
  • clinical uses:  ophtho. exams, shorter duration than atropine

Term
Ipratropium
Definition

  • class:  anticholinergic
  • type:  synthetic alkaloid derivative
  • receptor:  competitive inhibition of muscarinics
  • specific effects:  decrease bronchoconstriction and airway secretions
  • clinical uses:  asthma in cats, chronic bronchitis in dogs, recurrent airway inflammation in horses
  • note:  administer via inhalation to prevent side effects

Term
Propathelene
Definition

  • class:  anticholinergic
  • type:  synthetic alkaloid derivative
  • receptor:  competitive inhibition of muscarinics
  • specific effects:  detrusor relaxation, trigone, sphincter contraction
  • clinical uses:  urine retention (treat incontinence)

Term
Pancuronium
Definition

  • class:  NMJ blocker
  • type:  competitive, non-depolarizing
  • receptor:  nicotinic receptors at NMJ
  • effect:  muscle weakness, then flaccid paralysis
  • duration of action:  long (2-3 hours)
  • metabolism:  renal elimination (half-like increased with renal dz
  • toxicity issues:  little ganglionic blockade, no histamine release, blocks muscarinic receptors-tachycardia

Term
Atracurium
Definition

  • class:  NMJ blocker
  • type:  competitive, non-depolarizing
  • receptor:  nicotinic at NMJ
  • effect:  muscle weakness, then flaccid paralysis
  • duration:  intermediate (0.5-1 hour)
  • metabolism:  multiple modes of elimination (half-life not increased with renal disease); degradation reduced with hypothermia and acidosis
  • toxicity:  little/no ganglionic blockade, promotes histamine release

Term
Mivacurium
Definition

  • class:  NMJ blocker
  • type:  competitive, non-depolarizing
  • receptor:  nicotinic at NMJ
  • effect:  muscle weakness, then flaccid paralysis
  • duration:  short (15 min)
  • metabolism:  half-life not increased with renal disease
  • toxicity:  little/no ganglionic blockade, promotes histamine release

Term
Succinylcholine
Definition

  • class:  NMJ blocker
  • type:  non-competitive, depolarizing
  • receptor:  nicotinic at NMJ
  • effect:  early (phase I) depolarization with muscle fasciculations, late (phase II) with repolarization (receptor desensitization) and flaccid paralysis
  • duration:  short (1 min onset, 5 min duration)
  • toxicity:  no ganglionic blockade, some histamine release, hyperkalemia

Term
Epinephrine
Definition

  • class:  sympathomimetics
  • type:  direct-acting endogenous catecholamine
  • receptor:  alpha and beta
  • specific effects:
  • increases CO (beta-1)
  • peripheral vasoconstriction--increased BP at high dose (alpha-1)
  • skeletal mm. vasodilation and bronchodilation (beta-2)
  • clinical uses:  treat aanaphylaxis and asthma, restore cardiac rhythm, topical hemostasis, adjunct with local anesthetics

Term
Norepinephrine
Definition

  • class:  sympathomimetic
  • type:  direct-acting endogenous catecholamine
  • receptors:  beta-1 EPI=NE; beta-2 EPI>>>NE; alpha-1 EPI>NE
  • specific effects:  intense vasoconstriction, increased BP, no bronchodilation
  • clinical use:  maintain BP during shock (alpha-1, beta-1 effects)

Term
Dopamine
Definition

  • class: sympthomimetics
  • type:  direct-acting endogenous catacholamine
  • receptors:  vascular D1, cardiac beta-1, vascular alpha-1
  • specific effects:  low dose increase renal blood flow and Na excretion, positive inotropic effect; high dose vasoconstriction, decreased RBF
  • clinical uses:  low dose CRI for CHF with compromised renal function (short-term)

Term
Dobutamine
Definition

  • class:  sympathomimetics
  • type:  non-selective beta-adrenergic agonist
  • receptor:  beta-1>beta-2 and alpha-1 (closest to beta-1 selective agonist)
  • specific effects:  increase cardiac contractility with minimal change in HR and BP, bronchodilation
  • clinical uses:  inotrope during heart failure (short-term)
  • side effects:  unwanted/excess beta stimulation (increased HR when used as bronchodilator)

Term
Albuterol
Definition

  • class:  sympathomimetic
  • type:  selective beta-2 adrenergic agonist
  • receptor:  beta-2
  • specific effects:  bronchodilation
  • clinical uses:  bronchospasm in dogs, cats, horses
  • side effects:  unwanted/excess beta stimulation, cardiac excitation, receptor down-regulation

Term
Clenbuterol
Definition

  • class: sympathomimetic
  • type:  selective beta-2 adrenergic agonist
  • receptor:  beta-2
  • specific effects:  bronchodilation
  • clinical uses:  recurrent airway obstruction in horses
  • side-effects:  minimize with inhalation, proper dose and dosing schedule

Term
Phenylephrine
Definition

  • class: sympathomimetic
  • type:  selective alpha-1 adrenergic agonist
  • receptor:  alpha-1
  • specific effects:  vasopressor, decongestant
  • clinical uses:  increase BP, treat hypotension and shock
  • side-effects:  hypertension

Term
(Dex)medetomidine
Definition

  • class:  sympathomimetic
  • type:  selective alpha-2 adrenergic agonist
  • receptor:  alpha-2
  • specific effects:  CNS and presynaptic inhibition (decreases NE release)--sedation, analgesia
  • clinical uses:  adjunct for sedation, anesthesia, and analgesia (allows for lower doses of lower-safety agents)
  • note:  high safety profile

Term
Phenoxybenzamine
Definition

  • class:  sympatholytic
  • type: direct-acting non-competitive antagonist
  • receptor:  non-selective irreversible alpha antagonist
  • specific effects:  vasodilation, CNS excitation
  • clinical uses:  treat sympathomimetic-induced hypertension
  • note:  cannot be pharmacologically reversed, receptors must be replenished

Term
Phentolamine
Definition

  • class:  sympatholytic
  • type:  direct-acting competitive antagonist
  • receptor:  non-selective reversible alpha antagonist
  • specific effects:  vasodilation, CNS excitation
  • clinical uses:  treat sympathomimetic-induced hypertension

Term
Prazosin
Definition

  • class:  sympatholytic
  • type:  aelective alpha-1 adrenergic antagonist
  • receptor:  alpha-1
  • specific effects:  vasodilation, relax arterial and venous smooth mm.
  • clinical uses:  antihypertensive, used for CHF (decreases pre- and afterload)

Term

Atipamezole

Definition

  • class:  sympatholytic
  • type:  selective alpha-2 adrenergic antagonist
  • receptor:  alpha-2
  • specific effects:  increase sympathetic activity, decrease CNS inhibition (increase NE release)
  • clinical uses:  reversal of medetomidine sedation (antisedan)

Term
Propranolol
Definition

  • class:  sympatholytic
  • type:  non-selective beta-adrenergic antagonist
  • receptor:  beta-1 and beta-2
  • specific effects:  antiarrhythmic, increase bronchoconstriction
  • clinical uses:  decrease cardiac arrhythmias
  • generally not used due to beta-2 effects (bronchoconstriction)

Term
Timolol
Definition

  • class: sympatholytic
  • type:  non-selective beta-adrenergic antagonist
  • receptor:  beta-1 and beta-2
  • specific effects:  ocular use to decrease aqueous humor production
  • clinical use:  glaucoma

Term
Atenolol
Definition

  • class:  sympatholytic
  • type:  selective beta-1 adrenergic antagonist
  • receptor:  beta-1
  • specific effects:  decrease CO, HR, contraactility, BP; antiarrhythmic, decrease cardiac O2 demand
  • clinical uses:  feline hypertrophic cardiomyopathy

Term
Procainamide
Definition

  • class:  Na-channel blockers
  • type:  IA
  • receptor:  Na channels
  • effect:  moderate slowing of conduction velocity, lengthens refractory period
  • clinical use:  supraventricular tachycardia (from reentrant arrhythmia)

Term
Lidocaine
Definition

  • class:  Na-channel blocker
  • type:  IB
  • receptor:  inactivated Na channels
  • effect:  little change in conduction velocity, shortens refractory period
  • clinical use:  ventricular tachycardia (ectopic pacemaker)

Term
Flecainide
Definition

  • class: Na-channel blockers
  • type:  IC
  • receptor:  Na channels
  • effect:  large decrease in conduction, little change in refractory period
  • use:  use only in life-threatening situations (can be very arrhythmogenic)

Term
Atenolol, propranolol
Definition

  •  class: beta blockers (class II)
  • receptors:  beta-1 and beta-2
  • effect:  decreases sympathetic activity
  • clinical uses:  excessive sympathetic activity is arrhythmogenic, manage using beta-blockers

Term
Amiodarone
Definition

  • class:  action potential prolonging (class III)
  • receptors:  block K+ channels
  • effects:  prolong AP, increase refractory period
  • clinical uses:  reentrant supraventricular tachycardia
  • side effects:  arrhythmogenic, pulmonary fibrosis, derm problems

Term
Diltiazem, Verapamil
Definition

  • class:  Ca-channel blockers (class IV)
  • type:  non-vascular specific Ca-channel blockers
  • receptor:  Ca channels
  • effects:  slows AV node conduction
  • clinical use:  decrease ventricular response to atrial fibrillation
  • note:  can decrease cardiac contractility

Term
Digoxin
Definition

  • class:  miscellaneous antiarrhythmic
  • type:  similar action to class IV
  • receptors:  Ca channels
  • effects:  decrease AV node conduction
  • clinical use:  decrease ventricular response to atrial fibrillation
  • note:  very arrhythmogenic, AV block (must be tightly regulated)

Term
Adenosine
Definition

  • class:  miscellaneous antiarrhythmic
  • type:  ATP minus the TP
  • effects:  blocks AV node conduction
  • clinical use:  terminate supraventricular tachycardiacs involving SA node
  • note:  half-life=5 sec.

Term
Enalapril
Definition

  • class:  renin-angiotensin inhibitor
  • type:  ACE inhibitor
  • receptor:  competitive antagonist of ACE
  • mechanism:  prevents conversion of Ang I to Ang II
  • effect:  vasodilation

Term
Losartan
Definition

  • class:  renin-angiotensin inhibitor
  • type:  angiotensin receptor antagonist
  • receptor:  competitive antagonist of AT1 receptors
  • mechanism:  blocks pro-hypertensive effects of Ang II
  • side-effects:  decreases sympathetic activity, tubular water/Na retention (from decreased aldosterone), decreased water reabsorption (from decreased ADH)

Term
Amlodipine
Definition

  • class:  Ca-channel antagonist
  • type:  dihydropiridine
  • receptor:  vascular-specific Ca channel antagonist (not blocker!)
  • effects:  decrease arterial smooth mm Ca channel activity, decrease Ca entry and contraction of smooth mm.
  • clinical uses:  vasodilation, decrease TPR, temp increase of CO

Term
Nitroglycerin
Definition

  • class:  nitrovasodilator
  • type:  exogenous NO donor (stable organic nitrate)
  • effects:  venous dilation, arterial dilation at high doses
  • clinical uses:  cute cardiogenic pulmonary edema, CHF
  • note:  tolerance develops over time

Term
Sodium nitroprusside
Definition

  • class:  nitrovasodilator
  • type:  exogenous NO donor
  • effect:  arterial and venous dilation, decrease TPR, decrease BP
  • clinical uses:  hypertensive emergencies, acute CHF
  • note:  light sensitive--produces cyanide!!!  discard if dark brown, orange, blue

Term
Sildenafil (Viagra)
Definition

  • class:  PDE5 inhibitor
  • mechanism:  inhibition of PDE5 increases cGMP, increases PKG-->vasodilation
  • clinical uses:  manage pulmonary hypertension, BONERS!!

Term
Monoxidil
Definition

  • class:  K-channel activator
  • mechanism:  opens K channels in arterial smooth m.
  • effects:  hyperpolarize membranes, decrease Ca entry, decrease TPR, decrease BP
  • clinical use:  rarely used

Term
Hydralazine
Definition

class:  miscellaneous vasodilator

mechanism unclear

effects:  increase NO, increase cGMP, decrease IP3 induced Ca release

clinical uses:  hypertensice crises, reflex tachycardia, fluid retention

note:  use with diuretic in dogs with mitral insufficiency (decrease afterload)

Term
Milrinone
Definition

class:  PDE3 inhibitor

receptor:  PDE3 in myocardium

effects:  increase cAMP, increase PKA, increase Ca influx, increase Ca induced Ca release

clinical uses:  mimics effect of beta-1 stimulation, dhort-term use for acute heart failure, can be used with beta blockers

Term
Pimobendan
Definition

  • class:  calcium sensitizer
  • mechanism:  enhance contractile process directly by increasing affinity of troponin C for Ca
  • clinical use:  CHF in dogs
  • note:  only small increase in O2 consumption, not associated with arrhythmias

Term
Mannitol
Definition

  • class:  diuretic
  • type:  osmotic
  • mechanism:  overwhelms transporters ability to reabsorb molecule, increased osmotic pressure within lumen pulls water into tubules
  • clinical uses:  treat/prevent oliguric renal failure, cerebral edema, acute glaucoma
  • notes/side-effects:  do not use if can't establish renal flow or if intrcranial bleeding

Term
Acetazolamide
Definition

  • class: diuretic
  • type:  carbonic anhydrase inhibitor
  • location of action:  proximal tubule
  • mechanism:  increases loss of bicarb, increases urine pH
  • clinical uses:  treat metabolic alkalosis, glaucoma, altitude sickness
  • side effects/notes:  hypokalemia possible, alkalizing effect on urine can cause systemic acidosis

Term
Furosemide (Lasix, Salix)
Definition

  • class:  diuretic
  • type:  loop diuretic
  • location of action:  thick ascending limb of LOH
  • mechanism:  inhibits NaCl reabsorption, water follows urinary loss of NaCl
  • clinical uses:  treat oliguric renal failure, CHF, acute pulmonary hypertension, EIPH
  • notes/side-effects:  most effective diuretic, hypokalemia possible, may increase Ca loss in urine

Term
Chlorothiazide
Definition

  • class:  diuretic
  • type:  thiazide
  • location of action:  distal tubule
  • mechanism:  blocks NaCl reabsorption, may indirectly increase Ca reabsorption, reduces kidney stone formation
  • clinical uses:  nephrogenic diabetes insipidus, udder edema in cattle, Ca-containing uroliths
  • note:  not as effective as loops

Term
Spironolactone
Definition

  • class:  diuretic
  • type:  K-sparing
  • receptor:  mineralocorticoid receptor antagonist
  • mechanism:  competitive aldosterone antagonist; blocks aldosterone-induced expression of multiple genes, delays onset of action and prolongs effect
  • clinical uses:  milk diuresis with reduced potential for K loss, used in conjunction with loops

Term
Amiloride
Definition

  • class:  diuretic
  • type:  K-sparing
  • location of action:  epithelial Na channels
  • mechanism:  principle cell Na channel blocker
  • effect:  immediate, mild diuretic
  • used in conjunction with loops

Term
Triamterene
Definition

  • class:  diuretic
  • type:  K-sparing
  • location of action:  Na channels
  • mechanism:  principle cell Na channel blocker
  • used in conjunction with loops

Term

What is the primary mode of metabolism for NTs in the parasympathetic system?

 

What is the primary mode of metabolism for NTs in the sympathetic system?

Definition

para:  ACh is degraded by AChE

 

symp:  NE reuptake by adrenergic neuron (also uptake into effector cell)

Term
How do you monitor an NMJ block?
Definition

Train of Four:  stimulate superficial peripheral nerve four times and evaluate response of target muscle

 

if response is the same as before the block, need more drug

 

fade pattern with nondepolarizing block or late depolarizing block

 

constant but diminished pattern in early depolarizing block

Term
What are signs of NMJ toxicity?
Definition

  • respiratory paralysis
  • prolonged apnea and cardio collapse from histamine release or anaphylaxis
  • hypotension from ganglionic blockade
  • malignant hyperthermia (rare)--excessive contracture and heat production from skeletal muscle

Term
Basic types/causes of arrhythmias
Definition

disorders of impulse formation and/or conduction

 

pacemaker arrhythmias:

  • abnormal slowing of SA firing rate
  • abnormal acceleration of extopic firing rate

conduction arrhythmias:

  • bradycardia from AV nodal block
  • tachycardia from reentrant circuit

Term
Theoretical approaches to managing CHF include what two strategies?
Definition

reducing workload

increasing performance

Term
Positive ionotropic agents
Definition

sympathomimetics

dobutamine (beta-1, alpha-1)

dopamine (D1, beta-1)

 

PDE3 inhibitors

milrinone

 

cardiac glycosides

digoxin

 

calcium sensitizers

pimobendan

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