Comps Drugs Flashcards
Isoflurane
Forane
vapor pressure = 238mmHg
minimal cardio depression
HR increase 10-20%
Sevoflurane
Ultane
vapor pressure = 164mmHg
low solubility
cardio effects = mild neg inotropic effects, no tachy, CO not maintained like with ISO or DES
may prolong QT
slightly increases CBF & ICP, decreases CMRO2
degrade in soda lime to compound A (nephrotoxicity)
Desflurane
Suprane
vapor pressure = 664
boils @ room temp
low solubility (so rapid change in Parterial/Pbrain)
cardio = no steal, CO very slightly depressed, tachy, HTN
respiratory = slow/shallow breathing, airway irritation, breath holding, coughing.
CNS = increases CBF&ICP and decreased CMRO2
Halothane
Fluothane
sweet smelling
sensitizes myocardium to catecholamines to increased chance of arrhythmias
hepatotoxicity with high risk in fat females.
Brevital
Methohexital
Barbiturate
1mg/kg
interact with GABA to keep receptors open longer and increase duration of GABA activated Cl channels
Induces seizure activity but decreases duration
must be delivered with NaCL will precipitate with LR.
erebral vascular vasoconstriction – causes decreased cerebral blood flow and decreased cerebral blood volume
Sodium Thiopental
Barbiturate
3-5 mg/kg
interact with GABA to keep receptors open longer and increase duration of GABA activated Cl channels
residual CNS effects (hungover for hours)
More protein bound, more lipid soluble, metabolized slower
cerebral vascular vasoconstriction – causes decreased cerebral blood flow and decreased cerebral blood volume
Propofol
Diprivan
1.5-2.5 mg/kg
GABA agonist. increased Cl hyperpolarizes neuron and GABA stays around longer.
CNS = decrease CMRO2, CBF, ICP and CPP
CVS = decreased BP (vasodilaton), inotropic effect, HR.
Respiratory = decreased Vt, RR, vent response to CO2. bronchodilation and apnea
Etomidate
Amidate
0.2-0.3 mg/kg
GABA agoinist. hyperpolarizes neuron and GABA stays around longer
CNS = potent cerebral vasoconstrictor, decreases CBF, CMRO2, & ICP
CVS = cardiac stability (inhibits HR, SV and CO), decreases SVR, MAP, IOP
Respiratory = depressant decreases Vt but increases RR and apnea
adrenal cortical suppression
Ketamine
NMDA receptor antagonist
inhibits NMDA by glutamate so decreases presynapic release of glutamate
also affects opioid receptors MU2, Delta and Kappa
CNS = potent cerebral vasodilator (contraindicated if increased ICP) increased CBF, CMRO2 and amplitude of SSEP
CVS = increased BP, HR, CO and myocardial O2 requirements.
Respiratory = maintain SV, airway tone, bronchodilator
causes emergence delirium
Morphine
Onset = 15-30 min Peak = 45-90 min duration = 4hrs. Opioid Opioid receptor activation leads to decrease in neurotransmission
Meperidine
Demerol
Opioid
atropine like structure so causes tachy.
reduces post-op shivering
Codiene
Opioid
limited 1st pass hepatic metabolism so effective orally
cough suppressant
Sufentanil
Opioid
highly protein bound so lower volume of distribution
high lipid solubility so rapid penetration of BBB.
Very concentrated, dilution is required for accurate dosing
Afentanil
Opioid
rapid onset of action
ideal for brief stimulus
lower incidence of PONV (fentanyl and sufent)
Fentanyl
Sublimaze
1-2 mcg/kg for analgesia
100x as potent as morphine.
Onset = 6 minutes
long half time.
advantages = stable hemo, no myocardial depression or histamine release. supression of stress response
disadvantages = possible awareness, post-op vent depression
Remifentanil
Opioid
Profound respiratory depression when combined with propofol (but rapid recovery)
Can cause brady so supplement with robinul
Hydromorphone
Dilaudid
Opioid. Derivative of morphine
5x as potent as morphine and has a shorter duration
More sedation and less euphoria than morphine.
Methadone
Synthetic opioid agonist
Suppression of withdrawl symptoms for heroin addicts.
used in chronic pain due to long duration of action but accumulation can cause respiratory depression
Tramadol
Ultram
Opioid. moderate affinity for Mu, weak for delta and kappa.
Advantages = anelgesia w/o resp depression, low potential for dependence or abuse, no organ toxicity.
Disadvantages = seizures and interacts with coumadin
Naloxone
Narcan
Nonselective opioid antagonist (all 3 receptors) displaces agonist from receptor
short duration (30-40min) so may wear off before underlying narcotics.
Abrupt reversal or opioids can result in tachy, HTN, pulmonary edema, cardiac dysthymias and pain
Naltrexone
oral opioid antagonist
Ketorolac
Toradol NSAID. Nonselective COX inhibitor. Avoid in asthmatic patients because it blocks COX2 therefore blocking the prostaglandins (PGE2) that cause bronchodilation B --> bleeding A --> asthma A --> allergy to NSAIDS K --> kidney disease due to Na and H2O retention E --> extremes of age
Lorazepam
Ativan Benzo
Enhances GABA activity so hyperpolarizes cell reducing excitability
More potent than diazepam and midazolam
Slow onset and long duration of action
Treats severe anxiety disorders, insomnia and anti-convulsant
Midazolam
Versed Benzo
Enhances GABA activity so hyperpolarizes cell reducing excitability
Onset: 1-5 min, 1/2 life: 1-5 hours.
Dose: 0.5 mg/kg
Rapidly absorbed by GI so only 50% orally administered drug reaches systemic circulation due to first pass hepatic effect.
CNS: anticonvulsant, causes increase in ICP
Resp: decrease hyperactivity (a little bit)
CV: does not prevent increase in BP and HR to intubation.
Diazepam
Valium Benzo
Enhances GABA activity so hyperpolarizes cell reducing excitability
Insoluble in water so dissolved in propylene glycol so painful on injection.
Slower onset (55min) and prolonged duration (21-37hrs) than Versed
Oxazepam
Alepam Benzo
Enhances GABA activity so hyperpolarizes cell reducing excitability
Used for insomnia characterized by waking up in the middle o the night
Slow oral absorption
Clonazepam
Klonopin Benzo
Enhances GABA activity so hyperpolarizes cell reducing excitability
Good for controlling and preventing seizures.
Temazepam
Restoril Benzo
Enhances GABA activity so hyperpolarizes cell reducing excitability
Used only for treatment of insomnia.
No signs of tolerance or withdrawl.
Alprazolam
Xanex Benzo
Flumazenil
Romazicon Competitive benzodiazepine antagonist Reverses ventilatory depression Dose: 0.2 mg IV (10mcg/kg IV) Duration: 30-60 minutes
Succinycholine
Anectine depolarizng muscle relaxant
Resembles Ach so mimics it and binds to receptors and fills all of them so Ach can’t bind.
Diffuse away and broken down by pseudocholinesterase.
Onset: 30-60 seconds
Duration: 5-10 minutes
side effects MAD SHITS
Muscle soreness
Allergic Rxn
Dysrythmias
Sinus Tachy (adults due to stim of nicotinic rec at autonomic ganglia)
Hyper K
Increased ICP and IOP
Trismus
Sinus brady (peds due to muscarinic stim at sinus node)
Rocuronium
Zemuron steroidal NDMR
Competes for cholinergic receptors at the motor end-plate so Ach can’t bind. does not cause a depolarization.
Reversal depends on redistribution, metabolism and excretion.
Six times less potent than vec and has no active metabolite
Primarily eliminated by the liver.
Onset 1-2 minutes
Vecuronium
Norcuron steroidal NDMR
Competes for cholinergic receptors at the motor end-plate so Ach can’t bind. does not cause a depolarization.
Metabolized by deacetylation in the liver.
Pancuronium
Pavulon NDMR Competes for cholinergic receptors at the motor end-plate so Ach can't bind. does not cause a depolarization. Long duration of action 80% renal clearance can cause tachycardia.
Atracurium
Benzoisoquinolone NDMR
Competes for cholinergic receptors at the motor end-plate so Ach can’t bind. does not cause a depolarization.
Ester hydrolysis and spontaneous nonenzymatic Hoffman degredation
Causes histamine release
Cisatracurium
Nimbex Benzoisoquinolone NDMR
Competes for cholinergic receptors at the motor end-plate so Ach can’t bind. does not cause a depolarization.
Ester hydrolysis and spontaneous nonenzymatic Hoffman degredation
NO histamine release
Edrophonium
Anticholinesterase
Increases Ach at NMJ to compete with NDMR
Fast and complemented by Atropine
Weak hydrogen bonds (and electrostatic) so short duration of action
Onset: 1-2 minutes
Good test for Myasthemia gravis. If symptoms get better with 1mg then that is the diagnosis. (worsened symptoms means choinergic crisis)
Neostigmine
Prostigmin Anticholinesterase
Increases Ach at NMJ to compete with NDMR
complemented by glycopyrollate
Reversable ester bond (stronger and longer lasting than edrophonium)
onset: 7-11 minutes
Phyosigmine
Anticholinesterase
Increases Ach at NMJ to compete with NDMR
Crosses the BBB
Onset: 16 minutes with a long duration of action
Atropine
Anticholinergic Inhibits muscarinic receptor 2. M2 causes hyporolarization of myocyte. so atropine inhibits hyperpolarization increasing heart rate. Blocking parasympathetic stimulation Effects: Mad as a Hatter - neuro side effects crosses BBB Hot as a Hair - inhibition of sweating Red as a Beet - inhibition of sweating Blind as a Bat - pupillary dilation Dry as a Bone - decreased salivation
Scopolamine
Anticholinergic
Used for anti-nausea
more sedating and more potent antisalagogue than atropine
Causes less tachy
Glycopyrolate
Anticholinergic
Does not cross BBB (no neuro side effects)
Ipratropium
Atrovent
Anticholinergic Aerosol administration
combivent + albuterol
Acts mainly on the lungs so good for emphysema and bronchitis
Dopamine
Natural catecholamine Dopamine 1 receptor: vasodilation to increase renal BF and UOP, CO and cerebral BF Dopamine 2 receptor: inhibits release of NE 0.5 to 3 mcg/kg/min IV Dopamine-1 receptors Renal vascular dilation 3-10 mcg/kg/min IV Beta-1 in the heart >10 mcg/kg/min IV Alpha/Beta
Dobutamine
Selective beta-1 agonist
Used to improve CO in pts with heart failure
Used when Heart Rate and SVR are elevated
Combine with vasodilator to reduce afterload
Usually only small increase in Heart Rate (less effect than isoproteronol)
Isoproterenol
Synthetic catecholamine
No alpha effects but most potent activator of Beta 1 and 2 (2-10x epi and 100x as Norepi)
Used for
bronchodilation (more common to use a specific beta 2)
to increase heart rate (good for complete heart block)
to decrease pulmonary vascular resistance (pulmonary HTN)
Phenylepherine
Synthetic noncatecholamine
Directly stimulates Alpha-1 Adrenergic receptors
venoconstriction>arterial constriction
reduces BF to renal, splanchnic and cutaneous.
increases BF to coronaries
Ephedrine
Indirect-acting synthetic noncatecholamine that stimulates alpha and beta adrenergic receptors.
Indirect by endogenous release of NE
Tachyphylaxis with repeated doses.
Antiemetic effect 0.5mg/kg IM
Uterine blood flow is not altered (phenylepherine decreases)
Amphetamine
Indirect acting synthetic noncatecholamines
Endogenous NE released
Unlike ephedrine there is significant Central Nervous System stimulation and appetite suppression.
Theophylline
Selective Beta 2 agonist
bronchodilator
Used to treat acute severe exacerbation of asthma
Calcium
Noncatecholamine nonglycoside cardiac inotrope
Rapid inotropic effect that lasts 10-20 minutes
increases stroke volume and decreases LVEDP
Milrinone
Noncatecholamine nonglycoside cardiac inotrope
Positive inotrope and vasodilation
Inhibition of phosphodiesterase (increased cAMP)
Glucagon
Noncatecholamine nonglycoside cardiac inotrope
Produced by the pancreas
increases contractility and HR in presence of beta blocker
Phenoxybenzamine
Nonselective alpha antagonist
Irreversible and long acting (48 hrs)
Phentolamine
Nonselective alpha antagonist Reversible competitive blockade which can be overcome by increase in NE short acting (3-5hrs)
Prazosin
Minipress
Selective alpha 1 agonist
Oral taken at home for HTN , congestive heart failure, angina and arrhythmias..
Terazosin
Selective alpha 1 agonist
Less tachy, more selective and longer acting than prazonin.
For bladder relazation for BPH
Propanolol
nonselective beta antagonist (beta blockers)
First beta blocker, high protein bound and blocks clearance of amide LA’s,
Blocks Na channels so has some LA activity.
Timolol
nonselective beta antagonist (beta blockers)
used for glaucoma
Labetalol
Trandate
nonselective beta antagonist WITH alpha 1 antagonism (beta blockers)
Quick on and off
less brady
Carvedilol
nonselective beta antagonist WITH alpha 1 antagonism (beta blockers)
Used for HTN and CHF
Esmolol
Brevibloc
Selective beta 1 antagonist (beta blocker)
Quick on quick off (15 min total)
Metoprolol
Lopressor
Selective beta 1 antagonist (beta blocker)
Large doses become nonselective.
Atenolol
Selective beta antagonist (beta blocker)
Most selective B1.
For patients with CAD and MI risk
Clonidine
partial long acting a2 agonist
decreases SNS activity and causes some vagal stimulation (brady and dilation)
Reflex HTN if stopped
Decreases MAC
Sodium Nitroprusside
Nipride Nitric Oxide vasodilator
venous and arterial relaxation (lowers pre and afterload)
side effects –> coronary steal and reflex tachy
Nitroglycerine
Nitrol
Venous dilation only
Hydralazine
Apresoline
direct arterial vasodiator
decreases diastole more than systole.
reflex tachy (SNS from baroreceptors)
Quinidine
Na channel blocker class 1A so risk of torsades
slows conduction/depolarization, lengthens AP
Used for SVT, PVC, WPW
Procainamide
Na channel blocker (procane analogue) class 1A so risk of torsades
slows conduction/depolarization, lengthens AP
used for PVC and Vtach (NOT SVT)
Lidocaine
Na channel blocker class 1B so NO risk of torsades good for Vtach and PVC
Phenytoin
Dilantin
Na channel blocker 1B shortens QT so prevents torsades
Used for digitalis toxicity
Esmolol
Beta blocker. slows AV node and phase 4 depolarization
Sinus tachy, afib, torsades
block effective if between 55-65
Amiodarone
K channel blocker. prolongs repolarization and refractory period.
only drug that can prevent arrythmias!
noncompetitive B/a block, come Ca and Na channel block,
Causes dig toxicity
Diltiazem
Cardizem
Ca channel blocker
Selective to AV node and acts on Na/K pump
Verapamil
Calan
Ca channel blocker
Good for SVT and angina BUT can trigger WPW
AV node selective so avoid in pts with AV block
Digoxin
for a-fib
slows conduction by blocking Na/K ATPase which inhibits Na/Ca pump keeping more Ca in the cell increasing inotropy.
Adenosine
increases K currents (opens all the potassium channels) and shortens AP
Good alternative to Verapamil for SVT and it will not cause WPW
