Unit 06: drugs Flashcards

1
Q

what is yohimbine

A

Alpha 2 receptor antagonist

  • can reverse effects of alpha2 receptor agonists
  • drugs can reverse sedation and most cardiovascular effects
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2
Q

what is atipamezole

A

Alpha 2 receptor antagonist

  • can reverse effects of alpha2 receptor agonists
  • drugs can reverse sedation and most cardiovascular effects
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3
Q

what is dexmedetomidine

A

sedative

  • alpha-2 agonist
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4
Q
A
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5
Q

what is diazepam

A

sedative

benzodiazepine

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6
Q

what is medetomidine

A
  • mixture of 2 enantiomers - dexmedetomidine and levomedetomidine

(dexmedetomidine is the biologically active)

  • when ued at moderate dosages with general anesthetic there is usually no significant change in BP
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7
Q

what is flumazenil

A
  • GABA R antagonist: competitive inhibitor of benzodiazepine site
  • reverses overall effects of benzodiazepines
  • used to reverse benzodiazepine overdose
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8
Q

what is fentanyl

A

mu receptor agonist with intense analgesic effect, known as the “full Mu agonist”.

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9
Q

what is pentazocine

A

opioid

kappa agonist with good analgesic effect

also produces a weak effect at mu receptors, making it act like an antagonist to other mu opioids

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10
Q
A
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11
Q

what is loperamide?

A
  • reduce propsulive gut motility in large bowel, decrease gut secretions and cause constiction of anal spincter
  • stool remians in large colon longer which allows more water to be reabsorbed - potent constipating effect
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12
Q

what is Diphenoxylate?

A
  • reduce propsulive gut motility in large bowel, decrease gut secretions and cause constiction of anal spincter
  • stool remians in large colon longer which allows more water to be reabsorbed - potent constipating effect
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13
Q
A
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14
Q

Ether

A

early general anesthetic

  • inhalant introducted in 1846
  • demonstrated little respiratroy or cardiovascular depression and relatively non-toxic
  • does have pungent odour and expolsive properties
  • now used as starter fluid in combustion engines
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15
Q

chloroform

A

CHCl3

early general anesthetic

  • inhalant introducted in 1847
  • non pungent odor and non explosive
  • can be hepatotoxic resulting in severe cardiovascular depresion
  • was preferred inhalant until almost 1950
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16
Q

what is nitrous oxide

A
  • AKA laughing gas
  • weak CNS depressant, cannot produce general anesthesia even when 100% NO is administered
  • used to reduce amount of other inhalants requires, speeds up uptake of gas anesthetics
  • can be used of analgesia, no respiratory depression is assocaited with it suse as longa s you dont go above 50-60% which would dispalce O2 ausing asphyxiation
  • little effect on cardiovascular system at lower conc
  • adverse effects include increasing uptake of other anesthetics, and effects on GI system (formation of gas pockets causing bloating), N2O outflow can cause hypoxia during recovery
  • todau used in dental clinics, hospitals and few veterinary clinics to reduce amount of hydrocarbon anesthetic required
17
Q

what is cyclopropane?

A
  • early general anesthetic
  • used to be most populat
  • associated with explosions in operating room bc has flammable properties
18
Q

sodium pentobarbital

A
  • barbiturate that is effective and relatively safe if used with caution (narrow safty margin)
  • elimination of drug requries hepatic metabolism- metabolism is too slow in emergency situations
  • injectible anesthetic
19
Q

halogenated hydrocarbon anesthetics

A
  • isoflurance, sevoflurane and desflurane
  • all inhalants
20
Q

what is sodium thiopental

A
  • barbiturate adiminstered via IV
  • ultra short duration with rapid induction and recovery rate

The physiological effects on the CNS include dose dependent depression in 10-30 seconds, and unconsciousness for 1½ - 3 minutes.

If a partial dose is administered, it is likely to cause excitement as opposed to induction.

21
Q

what is propofol

A

one of the most popular intravenous anesthetics

  • offers sedation and anesthesia but has poor analgesic effects
  • mainly used for induction and has short duration (2-5min) so can be utilized during short painful procedures
  • premedation should be used first sot hat less propofol is needed for respiratory induction- resulting in less blood pressure depression
  • half life of drug increases with age so can be problematic in geriatirc patients
22
Q

what is propofol

A
  • one of most popular intravenous anesthetics
  • offers sedation and anestheria btu has poor analgesic effects
  • short duration of action, should also use a premedication so less propofol is needed (minimize effects of blood pressure depression
  • actcs by slowing dissocition of GABA from tis receptor- longer inhibition of action potentials
  • can cause apnea for 30-60sec and dose dependent respiratroy despression but not usually a problem
  • can cause dope dependent depression of blood rpessure causing peripheral vasodilation
23
Q

what is ketamine

A

dissociateive anesthetic, only IV anesthetic with analgesic properties

GABA and NMDA antagonist (GABA is inhibitory so if u ihibt that get inc SNS activity)

  • can increase HR and BP due to SNS stimulation, can use this to advantage in patietns in cardiovascular shock
  • can rise intracranial pressue causing seizures, hallucinations and excitment during recovery phase
  • use with diazepam to rpoduce rapid, smooth induction with little effect on cardiovascualr system

*never used alone

24
Q

what is dantrolene

A

administer is patietn is suspected to be experiencing malignant hyperthermia (potential effect of halothane)

25
Q

what is Haloethane

A
  • inhalant anesthetic
  • 25% is metabolized, hepatotoxic metabolites
  • can cause hypoxia and increased CO2 causing epinephrine release, deos not change HR but CO can decrease (reduces BP)
  • can cause arrhythmias due to sensitivity of the myocardium to epinephine
  • can depress thermoregulation resulting in hypothermia or malignant hyperthermia (very dangerous but need to ahve a genetic mutation for that)
  • can result in liver damage bc hepatotoxic
26
Q

what is isoflurane

A
  • most common anesthetic
  • alsmot no toxicity since very little is metabolized
  • low solubiltiy in tissues so moves in and out of bdoy quickly
  • causes less depression of CO than halothane but does ccase vasodilation which can result in dose dependent drop in blood pressure
  • post anesthetic hepatic necrosis has been reported in 1/500,000 pateints
  • less potent than halothane and has pungent odour (only real drawback)
27
Q

what is sevoflurane

A
  • Inhalant anesthetic
  • less stable than isoflurane, breaks fown when exposed to CO2 abosrbent in anestheic machine amkign it worse when the oxygen flow rate is low
  • as result nephrotoxic ocmound is release “compound A” (MOA somewhat unknwon)
  • human metbaolize up to 5% producing fluride ions that are released and thought to damage renal tubules, this sint supported by data
28
Q

what is tubocurarine

A
  • non depolarizing NM blocker
  • also idnuced histamine relase which lowers bp
29
Q

what is pancuronium

A

NM blocker agent

  • replaced tubocurarine but tends ot be vagolytic (inhibits pSNS signaling in the vagus nerve causing increased HR)
  • has been replaced with rocuronium, mivacurium and atracirium
30
Q

what are currently used NM blocker agents

A

rocuronium, mivacurium and atracurium

  • differ mainly in duration of action and route of elimination
31
Q

what is atracurium

A

NM blocker agent

  • used to prevent eye movement during ocular surgery
  • chemically similar to acetylcholine and competitively blocks nicotinic receptors at neuromuscular junction
  • causes intense relaxation or paralysis of voluntary muscle
  • intensity of effect depends on dose
  • safer than other non depolarizing blockers like tubucurauine and pancuronium and depolarizing blockers like succinyl chlone which is now barely used
32
Q

what is cisatracurium

A
  • same advantages of atracurium but less liekly to cause adverse effects
33
Q

what is procain

A
  • first cocaine substitute
  • main local anesthetic until lidocaine
  • known as Novocain and still used but less frequently
  • problem is that its an ester which is cleaved by plasma esterases and has a short duration of action (15-60min)

esters are more allergenic then amides but are sometimes still use wen rapid onset but short duration is desired

34
Q

what is lidocaine

A
  • most widely used local anesthetic
  • numerous routes of administration and applications
  • overdose can cause drowsiness or seizures, muscle twitching, possible cardiac arrest and death
  • usualy administered via injection and has duration of action of 30-60 min
  • onset following infiltration is approx 3 min
  • can aso be topical gel or topical spray
35
Q

what is bupivacaine

A
  • antoher widely used local anesthetic
  • slower onset (15min) but logner duration (2-4 hours)
  • longer effects come with greater cardiovascular toxicity if an IV bolus forms, can cause severe ventricular arrhythias
  • lecobupivacaine is the s(-) enantiomer and does not dsitribute well to CNS and heart
  • **levobupivacaine has replaced bupivacaine for regional, IV use in human medicine.