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377 Cards in this Set
- Front
- Back
|
MOA: decr aqueous humor synthesis due to vasoconstriction
SE: mydriasis, stinging do not use in closed-angle glaucoma |
epinephrine (alpha agonist effect)
|
|
|
decr aqueous humor synthesis
no pupillary or visual changes alpha agonist |
Brimonidine
|
|
|
decr humor secretion
no pupillary vision changes beta-blockers |
timolol
betaxolol carteolol |
|
|
decr aqueous humor secretion due to decr in bicarb
via inhibition of carbonic anhydrase no pupillary changes |
acetazolamide
|
|
|
incr outflow of aqueous humor
contract ciliary muscle and open trabecular meshwork Cholinomimetics |
pilocarpine - direct
carbachol - direct physostigmine, echothiphate - indirect |
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what cholinomimetic is used in emergencies to very effectively open meshwork into canal of Schlemm?
SE: miosis, cytoplasm |
pilocarpine
|
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what incr the outflow of aqueous humor?
|
Latanoprost
darkens color of iris (browning) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
MOA of opiods
|
act as agonists on opiod receptors
to modulate synaptic transmission open K+ channels close Ca2+ channels decr synaptic transmission inhibit release of ACh, NE, 5-HT, glutamate, substance P |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what is the clinical use of opiods?
|
pain
cough suppression (dextromethorphan) diarrhea (loperamide, diphenoxylate) acute pulmonary edema maintenance programs for addicts (methadone) |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
what toxicities w/ opiods?
|
addiction
RESPIRATORY DEPRESSION constipation/miosis - do not develop tolerance additive CNS depression CONTRAINDICATED in head injury |
|
|
MOA: decr aqueous humor synthesis due to vasoconstriction
SE: mydriasis, stinging do not use in closed-angle glaucoma |
epinephrine (alpha agonist effect)
|
|
|
decr aqueous humor synthesis
no pupillary or visual changes alpha agonist |
Brimonidine
|
|
|
decr humor secretion
no pupillary vision changes beta-blockers |
timolol
betaxolol carteolol |
|
|
decr aqueous humor secretion due to decr in bicarb
via inhibition of carbonic anhydrase no pupillary changes |
acetazolamide
|
|
|
incr outflow of aqueous humor
contract ciliary muscle and open trabecular meshwork Cholinomimetics |
pilocarpine - direct
carbachol - direct physostigmine, echothiphate - indirect |
|
|
what prostaglandin incr aqueous humor?
|
Prostaglandin PGF2a
darkens color opf iris (browning) |
|
|
what drug is a partial agonist at opiod mu receptors
agonists at kapp receptors? |
butorphanol
|
|
|
what is the clinical use of butorphanol
|
pain
causes less respiratory depression than full agonists |
|
|
toxicity of butorphanol
|
causes w/d if on full opioid agonist
|
|
|
very weak opiod agonist
inhibits serotonin and NE reuptake (works on multiple neuotransmitters) |
tramadol
for chronic pain similar to opioids but decr threshold for seizures |
|
|
mu receptors
|
supraspinal and spinal analgesia
resp depression miosis euphoria reduced GI motility physical dependence |
|
|
kappa receptor
|
primary spinal analgesia
miosis sedation, dysphoria psychomimetics |
|
|
delta receptor
|
analgesia and respiratory effects
|
|
|
what is the first line for tonic-clonic seizures?
|
phenytoin
carbamazepine valproic acid |
|
|
what is the 1st line for absence seizures
|
ethosuximide
|
|
|
what is the 1st line for status? (acute)
|
benzodiazepine
|
|
|
what is the first line for prophylaxis of status?
|
phenytoin
|
|
|
what is the MOA of phenytoin?
|
incr Na+ channel inactivation
Fosphenytoin for parenteral use |
|
|
what drug is used for trigeminal neuralgia?
|
carbamazepine -1st line
|
|
|
what drug is used for trigeminal neuralgia?
|
carbamazepine -1st line
|
|
|
what is the MOA of carbamazepine?
|
incr Na+ channel inactivation
|
|
|
what is the MOA of carbamazepine?
|
incr Na+ channel inactivation
|
|
|
what is the MOA of Lamotrigine?
|
block voltage-gated Na+ channels
|
|
|
what is the MOA of Lamotrigine?
|
block voltage-gated Na+ channels
|
|
|
what is the MOA of cabapentin?
|
designed as GABA analog but primarily inhibits HVA calcium channels
used for peripheral neuropathy bipolar disorder |
|
|
what is the MOA of gabapentin?
|
designed as GABA analog but primarily inhibits HVA calcium channels
used for peripheral neuropathy bipolar disorder |
|
|
what is the MOA of topiramate?
|
blocks Na+ channels, incr GABA action
|
|
|
what is the MOA of topiramate?
|
blocks Na+ channels, incr GABA action
|
|
|
what is the MOA of phenobarbital?
|
incr duration of GABAa action
|
|
|
what is the 1st line in pregnant women and children?
|
phenobarbital
|
|
|
what drug is used for myoclonic seizures?
|
valproic acid
|
|
|
what is the MOA of valproic?
|
incr Na+ inactivation
incr GABA concentration |
|
|
what is the 1st line for absence siezures?
|
ethosuximide
|
|
|
what is the MOA of ethosuximide?
|
blocks thalamic T-type Ca2+ channels
|
|
|
what is the MOA of benzos?
|
incr GABAa action by frequency
used for seizures of eclampsia-1st line to prevent seizures of eclampsia is MgSO4 |
|
|
MOA of tiagabine
|
inhibits reuptake
|
|
|
vigabatrin
|
irresversibly inhibits GABA transminase
incr GABA |
|
|
Levetiracetam
|
MOA unknown
may modulate GABA and glutamate release |
|
|
Tox of benzos?
|
sedation
tolerance dependence |
|
|
tox of carbamazepine
|
diplopia
ataxis blood dyscrasia (agranulocytosism, aplastic anemia), liver tox, teratogenesis, induction of cytc P450 SIADH Stevens-Johnson syndrome |
|
|
tox of ethosuximide
|
GI distress
fatigue headache urticaria stevens-johnson syndrome EFGH (Fatigue, GI, Headache) |
|
|
tox if phenobarbital
|
sedation
tolerance dependence induction of P450 |
|
|
tox of phenytoin
|
nystagmus
diplopia ataxia sedation gingival hyperplasia hirsutism megaloblastic anemia teratogenesis (fetal hydantoin syndrome) SLE-like syndrome induction of cytc P450 |
|
|
stevens-johnson syndrome
|
prodrome of malaise and fever followed by pupuric and erythematous macules (oral, ocular, genital)
skin lesions progress to epidermal necrosis and sloughling |
|
|
tox of valproic acid
|
GI distress
rare but fatala hepatotox (measure LFTs) neural tube defects in fetus tremor weight gain contraindicated in pregnancy |
|
|
tox of Lamotrigine
|
stevens-johnson synrome
|
|
|
tox of phenytoin
|
gingival hyperplasia
induce Cytc P450 SLE-like syndrome megaloblastic anemia hirsutism teratogen (fetal hydantoin syndrome) diplopia ataxia sedation nystagmus |
|
|
tox of topiramate
|
sedation
mental dulling kidney stones weight loss |
|
|
tox of gabapentin
|
sedation
ataxia |
|
|
MOA of phenytoin
|
use-dependent blockade of Na+
incr refractory period inhibit glutamate release from excitatory presynaptic neuron |
|
|
MOA of barbiturates
|
phenobarbital
pentobarbital thiopental secobarbital incr duration of Cl- opening decr neuron firing |
|
|
clinical use of barbs
|
sedative for anxiety, seizure, insomnia, induction of anethesia
|
|
|
clinical use of phenytoin
|
tonic-clonic seizures
Class IB antiarrythmics |
|
|
how do you treat a barbiturate overdose?
|
symptom management
|
|
|
what is the MOA of benzos?
|
faciliate GABAa action by incr frequency of Cl-channel opening
decr REM sleep most have long half-lives active metabolites |
|
|
what is the clinical use of benzos?
|
anxiety
spasticity status epilepticus detox night terrors sleepwalking general anesthetic hypnotic |
|
|
how do you treat benzo overdose?
|
flumazenil
|
|
|
what are the short-acting benzos
|
Triazolam
Oxazepam Midazolam highest addictive potential TOM Thumb |
|
|
anesthetics- principles
|
must be lipid soluble
drugs w/ decr solubility in blood = rapid induction and recovery times incr solubility in lipids = incr potency = 1/MAC |
|
|
MAC
|
minimal alveolar concentration at which 50% of pop is anesthetized
varies w/ age |
|
|
MOa of anesthetics on lungs
|
incr rate + depth of ventilation = incr gas tension
|
|
|
MOA of blood
|
incr blood solubility
incr blood/gas partition coefficienc incr solubility incr gas required to saturate blood slower onset of action |
|
|
MOA of tissue
|
AV concentration gradient incr
incr solubility incr gas required to saturate tissue = slower onset of action |
|
|
MOA of inhaled anesthetics
|
uknown
Halothane, enflurane, isoflurane NO etc |
|
|
effects of inhaled anesthetics
|
myocardial depression
resp depr nausea/emesis incr cerebral blood flow |
|
|
toxicity of MOAs
|
hepatotox
nephrotox proconvulsant malignant hyperthermia expansion of trapped gas |
|
|
thiopental
|
high potency
high lipid solubility rapid entry into brain induction of anesthesia and short surgical procedures terminated by rapid redistribution into tissue and fat decr cerebral blood flow |
|
|
benzos
|
Midazolam - most common drug for endoscopy
use adjunctively w/ gaseous anesthetics and nacrotics may cause severe posteroperative resp depression decr BP and amnesia |
|
|
Ketamine
|
dissociative anesthetic
blocks NMDA receptors CV stimulants cause disorientation, hallucination, bad dreams incr cerebral blood flow |
|
|
opiates
|
morphine, fentanyl used w/ other CNS depressants
|
|
|
propofol
|
used for rapid anesthesia induction and short procedures
less postoperative nausea than thipental potentiates GABAa |
|
|
local anesthetics = esters
|
procaine
cocaine tetracaine |
|
|
local anesthetics - amids
|
lidocaine
mepivacaine bupivacaine amides have 2 Is in name |
|
|
MOA of local anethestics
|
block Na+ channels by binding specific receptors on inner portion of channel
preferentially bind to activated Na+ channels so most effective in rapidly firing neurons tertiary amine local anesthetics penetrate membrane in uncharged form then bind to ion channels as charged form |
|
|
in infected (acidic) tissue
how much anesthetic is need? more or less |
MORE
|
|
|
order of nerve blockade
|
small diameter fibers > large diameter
myelinated fibers > unmyelinated overall size factor predominates over myelination small myelinated > small unmyelinated > large myelinated > large unmyelinated fibers |
|
|
order of loss
|
pain lose first > temp > touch > pressure lost last
|
|
|
what are local anesthetics used for?
|
minor surgical procedures
spinal anesthesia |
|
|
tox of local anesthetics
|
CNS excitation
severe cardiovascular tox (bupivacaine) hypertension hypotension arrythmias |
|
|
depolarizing NMJ blockers
|
succinylcholine
reversal of blockade Phase I (prolonged depolarixation) no antidote - blcok potentiated by cholinesterase inhibitors Phase II: antidote consists of cholinesterase inhibitors |
|
|
nondepolarizing NMJ Blockers
|
tubocurarine
atracurium mivacurium pancuronium vecuronium rocuronium competitive compete w/ ACj receptors reversal blockade -neostigmine, adrophonium, other cholinesterase inhibitors |
|
|
tx malignant hyperthermia
|
concomitant use of inhalation (except N2O) anesthetics + succinylcholine --> malignant hyperthermia
|
|
|
MOA of dantrolene
|
prevents release of Ca2+ from the SR of skeletal muscle
|
|
|
what Parkinson drugs agonize dopamine receptors?
|
bromocriptine/pergolide - ergot alkaloid, partial dopamine agonist
pramipexole ropinirole non-ergots are preferred |
|
|
incr dopamine
|
amantadine
may incr dopamine release used as antiviral against influenza A and rubella tox = ataxia |
|
|
prevents dopamine breakdown
|
selegiline - selective MAO type B inhibitos
entacapone/tolcapone (COMT inhibitors) - prevents L-dopa degradation thereby incr dopamine availability |
|
|
what curbs excess cholinergic activity
|
benztropine - antimuscarinic
improves tremor and rigidity but has little effect of bradykinesia for essential or familial tremors use a beta-blocker |
|
|
selectively inhibits MAO-B which preferentially metabolizes dopamine over NE and 5-HT thereby incr availability of dopamine
|
Selegiline
adjunctive agent to L-dopa may enhance the adversive effects of L-dopa |
|
|
L-dopa toxicity
|
arrhythmias from peripheral conversion to dopamine
long-term use can --> dyskinesia following administration akinesia btwn doses carbidopa-peripheral decarboxylase inhibitor incr bioavailability of L-dopa in brain and tolimit peripheral effects |
|
|
5-HT 1b-ad agonist
causes vasoconstriction inhibits trigeminal activation and vasoactive peptide release half-life <2 hrs |
Sumatriptan
|
|
|
what is the clinical use of sumatriptan
|
acute migraine, cluster headache attcks
|
|
|
tox of sumatriptan
|
coronary vasospasm
mild tingling contraindicated in pts w/ CAD or prinzmetal's angina |
|
|
what Alzheimer's drugs is an NMDA antagonist
helps prevent excitotoxicity mediated by Ca2+? |
Memantine
|
|
|
what are the SEs of memantine?
|
dizziness
confusion hallucinations |
|
|
what are the MOA of donepezil
galantamine, rivastgmine |
AchE inhibitors
tox: nausea, dizziness, insomnia |
|
|
what NTs are abnormal in Huntington's
|
Incr dopa
decr GABA and ACh |
|
|
Reserpine + tetrabenazine MOA
|
amine depleting
|
|
|
Haloperidol
|
dopamine receptor antagoinst
|
|
|
what drug incr presynaptic vesicular release
to relieve ADHD |
Methylphenidate (Ritalin)
|
|
|
tox of antipsychotics
|
highly lipid soluble
stored in body fat --> very slow to be removed from body EPS side effects endocrine side effects --> galactorrhea blocking muscarinic, alpha, histamine receptors |
|
|
high potency antipsychotics
|
haloperidol
trifluoperazine fluphenazine more likely to cause EPS/neurologica side effects |
|
|
lower potency antipsychotics
|
thioridazine
chlorpromazine nonneuro SEs: anticholinergic, antihistamine SEs |
|
|
stereotypic oral-facial mvmts due to long-term antipsychotic use
often irreversible |
tardive dyskinesia
|
|
|
think FEVER for neuroleptic malignant syndrome
|
FEVER
Fever Encephalopathy vital unstable elevated nezymes rigidity of muscles rigidity, myoglobinuria, autonomic instability, hyperpyrexia |
|
|
Chlorpromazine -->
|
corneal despoits
thioridazine retinal deposits |
|
|
EPS side effects
|
4 hr acute dystonia
4 d akinesia 4 wk akathisia 4 mo tardive dyskinesia |
|
|
what is dystonia?
|
muscle spasm stiffness
oculogyric crisis |
|
|
akinesia
|
parkinsonian symptoms
|
|
|
akinesia
|
parkinsonian symptoms
|
|
|
akathisia
|
restlessness
inability to sit or stand in one position onset of akathisia can be complication |
|
|
tardive dyskinesia
|
stereotypic oral-facial mvmts due to long-term antypsychotic use
often irreversible |
|
|
what are the atypical antipyschotics
|
olanzapine
clozapine quetiapine risperidone aripiprazole ziprasidone |
|
|
MOA of atypical antipsychotics
|
block 5HT2, alpha, H1, doapmine receptors
|
|
|
what is the clinical use of atypical antipsychotics?
|
schizophrenia
OLANZAPINE - used for OCD, anxiety disorder, depression, mania, Tourette's syndrome |
|
|
tox of atypical antipsychotics
|
fewer extrapyramidal and anticholinergic side effects than traditional antipychostics
|
|
|
olanzapine and clozapine may cause what side effect?
|
weight gain
clozapine also causes agranulocytosis -must weekly monitor WBC |
|
|
lithium
|
not established
possibly related to inhibition of phosphoinositol cascade |
|
|
clincial use of lithium
|
mood stabilizer for bipolar disorder
blocks relapse and acute manic events used for SIADH |
|
|
what are the side effects of lithium?
|
tremors
hypothyroidism polyuria nephrogenic DI narrow therapeutic window sedation, edema, heart block |
|
|
lithium SEs
|
mvmt (tremor)
nephrogenic diabetes insipidus hypothyroidism pregnancy problems |
|
|
MOA of buspirone
clinical use? |
stimulates 5-HTa1 receptors
use: generalized anxiety disorder does not cause sedation, addiction, tolerance does not interact w/ alcohol |
|
|
name the TCAs
|
imipramine
amitriptyline desipramine nortriptyline clomipramine doxepin amoxapine |
|
|
MOA of TCAs
|
block reuptake of NE and serotonin
|
|
|
what can be used for bedwetting?
|
imipramine
|
|
|
what can be used for OCD?
|
clomipramine
|
|
|
fibromyalgia?
|
TCAs
also used for major depression |
|
|
side effects of TCAs
|
sedation
alpha-blocking effects atropine-like side effects tertiary TCAs have more anticholinerfic effects desipramine is least sedating has lower seizure threshold causes tachy and urinary retention (anticholinergic) |
|
|
Tri-Cs of TCAs
|
CONVULSIONS
COMA CARDIOTOX (arrhythmias) respiratory depr hyperpyrexia confusion/hallucination in elderly due to anticholinergic side effects |
|
|
how do you treat CV tox due to TCAs?
|
NaHCO3
|
|
|
what is the MOA of SSRIs?
|
fluoxetine
paroxetine sertraline citalopram |
|
|
use of serotonine-specific reuptake inhibitors
|
depression
OCD bulimia social phobias |
|
|
toxicities of SSRIs
|
serotonin syndrome w/ MAO inhibitors
hyperthermia muscle rigidity CV collapse flushing diarrhea seizures |
|
|
tx of SSRIs
|
Cyproheptadine (5HT2 receptor antagonist)
normally takes 2-3 weeks for antidepressant to have an effect |
|
|
SNRIs
|
Venlafaxine
duloxetine |
|
|
what is the MOA of SNRIs?
|
inhibit serotonin and NE reuptake
|
|
|
what is the clinical use of SNRIs?
|
depression
Venlafaxine -generalized anxiety disorder duloxetine indicated for diabetic peripheral neuropathy, greater effect on NE |
|
|
toxicity of SNRIs
|
incr BP
also stimulant effects, sedation, nausea |
|
|
monoamine oxidase inhibitors
|
phenelzine
traylcypromine isocarboxacid selegiline (selective MAO-B inhibitors) |
|
|
what is the clinical use of MAOIs?
|
atypical depression
anxiety hypochondriasis |
|
|
what is the tox of MAO inhibitors/
|
hypertensive crisis w/ TYRAMINE ingestion (wine and cheese) and beta-agonists
CNS stimulation Contraindicated w/ SSRIs or meperidine to prevent serotonin synrome |
|
|
bupropion
|
smoking cessation
incr NE and dopamine tox: stimulant effects, headache, seizures, bulimic pts no sexual SEs |
|
|
mirtazapine
|
alpha2 antagonist
incr release of NE and serotonin potent 5HT2 and 5HT3 receptor antagonist tox: sedation, incr appetite, weight gain, dry mouth |
|
|
maprotiline
|
blocks NE reuptake
tox: sedation, orthostatic hypotension, tox: sedation, nausea, priapism postural hypertension due to male-specific side effects |
|
|
what drugs do you ALKALINIZE the urine to treat overdose?
|
weak acids
phenobarbital methotrexate TCAs aspirin trapped in basic environments treat OD w/ bicarbonate |
|
|
what drugs do you ACIDIFY urine in OD?
|
amphetaminse
tx w/ ammonium |
|
|
what does phase I metabolism do?
|
reduction
oxidation hydrolysis yields slightly polar, water-soluble metabolites (often still active) |
|
|
Phase I enzyme
|
cytc P450
|
|
|
Phase II metabolism
|
acetylation
glucoronidation sulfation (GAS) VERY polar, inactive metabolites, renally excreted Conjugation-geriatric patietns lose phase I first |
|
|
what drugs do you ALKALINIZE the urine to treat overdose?
|
weak acids
phenobarbital methotrexate TCAs aspirin trapped in basic environments treat OD w/ bicarbonate |
|
|
what drugs do you ACIDIFY urine in OD?
|
amphetaminse
tx w/ ammonium |
|
|
what does phase I metabolism do?
|
reduction
oxidation hydrolysis yields slightly polar, water-soluble metabolites (often still active) |
|
|
Phase I enzyme
|
cytc P450
|
|
|
Phase II metabolism
|
acetylation
glucoronidation sulfation (GAS) VERY polar, inactive metabolites, renally excreted Conjugation-geriatric patietns lose phase I first |
|
|
maximal effect a drug can produce is
|
EFFICACY
|
|
|
amount of drug needed for a given effect is
|
POTENCY
|
|
|
competitive antagonist shifts curve to the right
causing |
decrease in potency and incr EC
need higher concentration to produce a given effect |
|
|
noncompetitive antagonists shifts curve downward
|
decr efficacy
|
|
|
partial agonist
|
lower maximal efficacy
potency is independent factor |
|
|
competitive antagonist shifts curve to the right
causing |
decrease in potency and incr EC
need higher concentration to produce a given effect |
|
|
sweat glands post/pre
|
Ach N
Ach M but SYMPATHETIC |
|
|
noncompetitive antagonists shifts curve downward
|
decr efficacy
|
|
|
cardiac and smooth muscle gland cells nerve terminal - sympathetic
|
Ach N
NE alpha and beta |
|
|
partial agonist
|
lower maximal efficacy
potency is independent factor |
|
|
sweat glands post/pre
|
Ach N
Ach M but SYMPATHETIC |
|
|
cardiac and smooth muscle gland cells nerve terminal - sympathetic
|
Ach N
NE alpha and beta |
|
|
adrenal medulla
|
Ach N
Epi NE released by adrenal medulla |
|
|
renal vascular SM
|
Ach N
D1 |
|
|
PNS skeletal muscle
|
ACh N
|
|
|
Muscarinic Ach receptors are
|
G-protein coupled receptors that act through 2nd messengers M1-M5
|
|
|
Nictotinic Ach receptors
|
ligant-gated Na+/K+ channels
Nn in ANS ganglion Nm in neuromuscular junction |
|
|
what receptors are Gq?
|
H1
alpha1 V1 M1 M3 HAVe 1 M&M |
|
|
signaling cascade of Gq
|
receptor --> PLC --> lipids --> PIP2 --> IP3 --> Ca2+ and DAG --> PKC
|
|
|
what receptors are Gs?
|
b1, b2, D1, H2, V2
|
|
|
what receptors are Gi?
|
M2, a2, D2
|
|
|
Gs cascade
|
receptor --> AC --> ATP--> cAMP --> PKA
|
|
|
Gi receptor cascade
|
inhibit AC --> decr camp--> decr PKA
|
|
|
what cholinomimetic is used for postoperative and neurogenic ileus and urinary retention?
|
BETHANECHOL
activates bowel and bladder SM resistant to AChE Beth Anne, call me if you want to active your bowels and bladder |
|
|
what cholinomimetic is used for glaucoma, pupillary contraction, release of IOP
|
Carbachol
|
|
|
what is a potent stimulator of sweat, tears, saliva?
|
Pilocarpine-1st choice
contracts ciliary muscle of eye (open angle) pupillary sphincter (narrow angle) resistent to AChE PILE On the sweat and tears CAN ENTER CNS! |
|
|
challenge test for diagnosis of asthma
|
methacholine
stimulates muscarinic receptors in airway when inhaled |
|
|
what is used to diagnose MG? short acting
|
edrophonium
|
|
|
what 2 indirect agonists are used GLAUCOMA
|
physostigmine-cross BBB, atropine OD
echothiphate -glaucoma |
|
|
what is used for postoperative neurogenic ileus and urinary retention, myasthenia gravis-reversal of NMJ blockade
|
neostigmine
|
|
|
what is used to treat MG?
|
pyridostigmine
|
|
|
CHolinesterase inhibitor poisoning causes what sx?
|
Diarrhea
Urination Miosis Bronchospasm BRady Excitation of SM and CNS Lacrimation Sweating Salivation abdominal cramping |
|
|
what is the antidote for cholinesterase inhibitor poisoning?
|
atropine muscarinic antagonist
palidoxime to regenerate active cholinesterase |
|
|
what produces mydriasis and CYCLOPLEGIA
|
atropine
homatropine tropicamide Belladonna huge eyes |
|
|
what is used for Parkinson's disease, antimuscarinic
|
Benztropine
|
|
|
what is used for motion sickness?
|
Scopolamine
|
|
|
what is used for respiratory asthma COPD
|
ipratropium
|
|
|
what is used for GU -reduce urgency in mild cystitis and reduce bladder spasms?
|
oxybutynin
glycopyrrolate |
|
|
what is used for peptic ulcer treatment?
|
Methscopolamine
propantheline |
|
|
atropine
|
blocks DUMBBELSS
incr body temp, rapid pulse, dry mouth, fry flushed skin cycloplegia constipation disorientation can cause angle-closure glaucoma in elderly urinary retention in men w/ prostatic hyperplasia hyperthermia in infants |
|
|
SE of atropine
|
Hot as a hare
Dry as a bone Red as a beet Blind as a bat Mad as a hatter |
|
|
nictoinic antagonist
ganglionic blocker used in experiments to prevent vagal reflex responses to changes in BP prevents reflex bradycardai caused by NE |
Hexamethonium
tox: severe orthostatic hypotension blurred vision, constipation, sexual dysgunction |
|
|
epinephrine
|
a1, a2, b1, b2
low doses selective beta1 (blow) anaphylaxis glaucoma asthma hypotension |
|
|
NE
|
a1, a2 >b1
decr Renal perfusion - |
|
|
isoproterenol
|
b1=b2 isolated to b
AV Block (rare) |
|
|
dobutamine
|
b1>b2
inotropic but not chronotropic |
|
|
ritodrine
|
b2
reduces premature uterine contractions |
|
|
what sympathomimetics are beta2 selective?
|
MAST
metaproterenol Albuterole for acute asthma Salmeterol for long term Terbutaline to reduce premature uterine contractions |
|
|
amphetamine MOA
|
indirect general agonist, releases stored catecholamines
used for narcolepsy, obesity, ADHD |
|
|
ephedrine MOA
|
causes indirect general agonist
releases stored catecholamines USED FOR: nasal decongestion, urinary incontinence, hypotension |
|
|
cocaine MOA
|
indirect general agonist
uptake inhibitor causes vasoconstriction and local anesthesia |
|
|
what is the MOA of guanethidine?
|
antihypertensive
blocked NE release |
|
|
MOA of clonidine and methyldopa?
|
centrally acting a2 agonists
decr central adrenergic outflow for : hypertension, esp renal disease |
|
|
what are nonselective a-blockers?
|
phenoxybenzamine- irreversible
phentolamine (reversible) |
|
|
what are nonselective a-blockers used for?
|
pheochromocytomas, rayndauds, peripheral vascular disease
tox: orthostatic hypotension and reflex tachy |
|
|
what are a1 selective blockers?
|
-zosins
used for HTN and BPH tox: 1st dose orthostatic hypotention, dizziness, headache |
|
|
what are a2 selective blockers?
|
mirtazapine
used for depression tox: sedation, incr serum cholesterol, incr appetite |
|
|
epi + alpha blockade
|
decr BP to below baseline
|
|
|
phenyephrine + alpha blockade
|
suppress BP to baseline
|
|
|
what are beta blockers used for?
|
HTN
angina MI SVT - propranolol/esmolol by decr AV conduction velocity CHF slows pregression of chronic failure glaucoma- decr secretion of aq humor |
|
|
tox of beta blockers
|
impotence
exacerbation of asthma CV adverse effect CNS adverse effects use w/ caution in diabetics |
|
|
what are b1 selective?
|
A BEAM of b1 blockers
betaxolol esmolol atenolol metoprolol |
|
|
partial beta-agonists
|
PINDOLOL
ACEBUTOLOL |
|
|
nonselective beta antagonists
|
propranolol
timolol nadolol pindolol labetaolol |
|
|
antidote for antimuscarinig, anticholinergic agents
|
PHysostigmine salicylate
|
|
|
antidote for iron
|
deferoxime
|
|
|
antidote for lead
|
CaEDTA
dimercaprol succimer penicillamine |
|
|
antidote for mercury, gold, arsenic
|
dimercaprol
succimer |
|
|
copper arsenic gold antidote
|
penicillamine
|
|
|
antidote for cyanide
|
nitrite, hydroxocobalamin
thiosulfate |
|
|
antidote for methemoglobin
|
methylene blue
vitamine C |
|
|
antidote for CO
|
100% o2, hyperbaric o2
|
|
|
antidote for methanol, erthylene glycol
|
ethanol
dialysis fomepizole |
|
|
antidote for TCAs
|
slkalnize serum w/ NaHCO3
|
|
|
antidote for heparin
|
protamine
|
|
|
antidote for warfarin
|
vit K
fresh frozen plasma |
|
|
antidote for tPA streptokinase
|
aminocaproic acid
|
|
|
antidote for theophylline
|
betablocker
|
|
|
what drug causes atropine-like side effects?
|
TCAs
|
|
|
antidote for heparin
|
protamine
|
|
|
antidote for warfarin
|
vit K
fresh frozen plasma |
|
|
antidote for tPA streptokinase
|
aminocaproic acid
|
|
|
antidote for theophylline
|
betablocker
|
|
|
what drug causes atropine-like side effects?
|
TCAs
|
|
|
what drugs can cause coronary vasospasms
|
cocaine
sumatriptan |
|
|
what causes torsades de pointes
|
Class III (sotalol)
Class IA (quinidine) antiarrhythmics cisapride |
|
|
what causes dilated cardiomyopathy?
|
daunorubicin
doxorubicin |
|
|
cutaneous flushing
|
VANC
vancomycin adenosine niacin calcium channel blockers |
|
|
agranulocytosis
|
clozapine
carbamazepine colchine propylthiouracil/methimazole dapsone |
|
|
aplastic anemia
|
chloramphenicol
benzene NSAIDs propylthiouracil/mthimazole |
|
|
positive for direct coombs + hemolytic anemia
|
methyldopa
procainamide quinidine penicillamine |
|
|
gray baby syndrome
|
chloramphenicol
|
|
|
hemolysis in G6PD def pts
|
isoniazid
sulfa primaquine aspirin ibuprofen nitrofurantoin |
|
|
megaloblastic anemia
|
phenytoin
methotrexate sulfa drugs |
|
|
acute cholestatic hepatitis
|
macrolides
|
|
|
focal to massive hepatic necrosis
|
halothane, valproic acid
acetaminophen amanita phalloids |
|
|
hepatitis
|
INH
|
|
|
pseudomembranous colitis
|
clindamycin
ampicillin |
|
|
adrenocortical insufficiency
|
glucocorticoid w/d HPA suppression
|
|
|
gynecomastia
|
Some Drugs Create Awesome Knockers
Spironolactone Digoxin Cimetidine chronic Alcohol Use estrogens Ketoconazole |
|
|
hot flashes
|
tamoxifen
clomiphene |
|
|
hypothyroidism
|
lithium
amiodarone |
|
|
gout
|
thiazides, furosemide
|
|
|
photosensitivity
|
sulfonamides
amiodarone tetracycline SAT for a photo |
|
|
Rash (steven-johnson syndrome)
|
Ethosucimide,
Lamotrigine Carbamazepine phenobarb phenytoin sulfa drugs penicillin allopurinol |
|
|
SLE-like syndrome
|
Hydralazine
INH Procainamide Phenytoin |
|
|
Fanconi's
|
expired tetracycline
|
|
|
interstitial nephritis
|
methicillin
NSAIDs furosemide |
|
|
hemorrhagic cystitis
|
cyclophosphamide
ifosfamide - prevent coadministrating w/ mesna |
|
|
cinchonism
|
quinidine
quinine |
|
|
DI
|
lithium
demeclocyline |
|
|
parkinson-like syndrome
|
haloperidol
chlorpromazine reserpine metoclopramide |
|
|
seizures
|
bupropion
imipenem/cilastatin isoniazid |
|
|
tardive dyskinesia
|
antipsychotics
|
|
|
disulfiram like reaction
|
metronidazole
certain cephalosporins procarbazine 1st generation sulfonylureas |
|
|
nephro and neuro tox
|
polymyxin
|
|
|
nephro and ototox
|
AG
vanco loop cisplatin |
|
|
inducers +
|
quinidine
barbs st. john's wort phenytoin rifampin griseofluvin carbamazepine chronic alcohol use |
|
|
inhibitors -
|
sulfonamide
isoniazid cimetidine ketoconazole erythromycin grapefruit juice acute alcohol use |
