Neural pharmacology Flashcards
how does epinephrine treat glaucoma
decreases aqueous humor production via vasoconstriction
name an alpha 2 agonist that treats glaucoma
brimonidine
what are the side effects of using epinephrine to treat glaucoma
mydriasis (so do not use in close-angle glaucoma)
what are the side effects of brimonidine
ocular allergic reactions and blurry vision
what beta blockers are used to treat glaucoma
timolol, betaxolol, and carteolol
how does acetazolamide treat glaucoma
decreases aqueous humor by inhibiting carbonic anhydrase
which direct cholinomimetics treat glaucoma and what are their side effects
pilocarpine and carbachol;
side effects= miosis and cyclospasm (from contraction of the ciliary muscle)
how do direct cholinomimetics treat glaucoma
increase aqueous humor outflow by contracting ciliary muscle and opening of trabecular meshwork
name two indirect cholinomimetics that treat glaucoma
physostigmine and echotiophate
how do indirect cholinomimetics treat glaucoma
open trabecular meshwork to absorb aqueous humor
what prostaglandin is used to treat glaucoma and how does it work
latanoprost (PGF-2alpha); works by increasing outflow of aqueous humor
what is the side effect of latanoprost
darkening of the iris
list as many opioid analgesics as you can
morphine, fetanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate
by what mechanism do opioid analgesics work
they bind and stimulate opioid receptors (mu, delta and kappa) in order to open K+ channels and close Ca2+ channels —> decreased synaptic transmission —> inhibits release of ACh, serotonin, NE, glutamate and substance P (a neuromodulator)
what are opioid analgesics used for
pain, cough suppression (dextromethorphan), diarrhea (loperamide and diphenoxylate), acute pulmonary edema, maintenance programs for heroin addicts (methadone)
what are the side effects of opioid analgesics
addiction, respiratory depression, constipation, miosis, additive CNS depression with other drugs;
Note: tolerance does not develop to miosis and constipation
what is the antidote for opioid analgesics
naloxone or naltrexone (opioid receptor antagonists)
name the three opioid receptors and what they respond to
mu-opioid = morphine delta= enkephalin (regulates nociception by inhibiting pain) kappa= dynorphin (another pain modulator)
what two receptors does butorphanol act on and with what relative efficacy
butorphanol is a kappa full agonist and mu partial agonist
what is butorphanol used for and what makes it better than the alternative choices
severe pain (headaches, labor) less respiratory depression
what are the toxicities of butorphanol
withdrawl if taken with a full opioid agonist; not easily reversed with naloxone
what does tramadol treat and how does it work
tramadol treats chronic pain;
works as a weak opioid agonist and also as a reuptake inhibitor for 5-HT and NE.
what are the toxicities of tramadol
decreases seizure threshold and can cause serotonin syndrome
list all the epilepsy drugs
“ECG TTVV LLPP Benzos”:
ethosuximide, carbamazepine, gabapentin, topiramate, tiagabine, valproic acid, vigabatrin, lamotrigine, levetiracetam, phenytoin, phenobarbitol, benzodiazepines (diazepam and lorazepam)
what kind of seizure is ethosuximide used for and how does it work
absence; ethosuximide blocks thalamic T-type Calcium channels
what are the side effects of ethosuximide
EFGHIJ: Ethosuximide causes Fatigue, Gastrointestinal upset, Headache, Itching (urticaria), and steven-Johnson syndrome
what kind of seizure are benzodiazepines used for and how do they work
status epilepticus; they work by increasing GABA-A action
what are the side effects of benzodiazepines
sedation, dependence, tolerance, respiratory depression
what is first line treatment for ecclampsia seizure? second line treatment?
1st line= MgSO4
2nd line= benzodiazepines
what kinds of seizure does phenytoin treat
simple and complex
1st line for tonic-clonic
prophylaxis for status epilepticus
how does phenytoin work
sodium channel inactivation
what ind of kinetics does phenytoin exhibit
zero-order
what are the side effects of phenytoin
face: nystagmus, ataxia, diplopia, hirsutism, gingival hyperplasia
systemic: megaloblastic anemia, teratogenesis (fetal hydantoin syndrome), SLE-like syndrome, induction of CYP-450, LAD
skin/bone: osteopenia, Steven-Johnson syndrome
how is phenytoin given parenterally
fosphenytoin
for what 3 kinds of seizures is carbamazepine 1st line therapy
simple partial, complex partial, and tonic-clonic
how does carbamazepine work
sodium channel inactivation
what are the side effects of carbamazepine
diplopia, ataxia, blood dyscrasias (such as agranulocytosis and aplastic anemia), hepatotoxicity, teratogenesis, induction of CYP-450, SIADH, Stevens-Johnson syndrome
what is valproic acid used for
1st line for simple partial, complex partial and absence
1st line acute treatment for: tonic-clonic seizures
what 3 drugs are used as 1st line acute therapy for tonic-clonic seizures
phenytoin, carbamazepine and valproic acid
what drug is 1st line treatment for trigeminal neuralgia
carbamazepine
how does valproic acid work
sodium channel inactivation;
inhibiting GABA transaminase in order to increase GABA concentration
what are the toxicities of valproic acid
GI upset, hepatotoxicity, spina bifida in fetus (contraindicated in pregnancy), tremor, weight gain
what are the other uses of valproic acid
myoclonic seizures and bipolar disorder
what kinds of seizures does gabapentin treat
simple, complex and tonic-clonic
how does gabapentin work
inhibits high-voltage Ca2+ channels; GABA analog
what are the non-epileptic conditions that gabapentin is used for
peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis, bipolar disorder
what kind of seizure does phenobarbitol treat
simple, complex and tonic-clonic
how do barbituates work
facilitate GABA-A action by increasing duration that Cl- channel is open, thereby decreasing neuron firing
how do lamotrigine and topiramate work
block Na+ channels
what drugs treat simple, complex and tonic-clonic seizures
phenytoin (1st line tonic-clonic) carbamazepine (1st line for all three) gabapentin phenobarbital topiramate levetiracetam lamotrigine (plus absence)
what drugs treat only simple and complex seizures and how do they work
tiagabine and vigabatrin;
they work by increasing GABA levels
what is Steven Johnson syndrome
prodrome of malaise and fever followed by erythematous, purpuric macules (oral, ocular and genital) that become necrotic and slough off
for what condition are barbituates contraindicated
porphyria
what are barbituates used for
sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)
what are the side effects of barbituates
cardiac and respiratory depression, CNS depression, dependence, drug interactions (induces CYP-450)
name as many benzodiazepines as possible
lorazepam, diazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alprazolam
how do benzodiazepines work
they increase the frequency of Cl- channel opening
what are benzodiazepines used for
anxiety, spasticity, status epilepticus, alcohol detox, night terrors, sleepwalking, general anesthesia, insomnia
which is safer for your airway: barbituates or benzodiazepines
benzodiazepines
what are the side effects of benzodiazepine
dependence, additive CNS depression with alcohol
what drug is used to treat benzo overdose
flumazenil (competitive antagonist at GABA benzodiazepine receptor)
name three nonbenzodiazepine hypnotics
zolpidem (ambien), zaleplon, eszopiclone
how do nonbenzodiazepine hypnotics work and how are they reversed
act on the BZ1 subtype GABA receptor;
reversed by flumazenil
what is minimal alveolar concentration
concentration at which 50% of patients will move in response to noxious stimuli
name as many inhales anesthetics as you can
halothane, isoflurane, enflurane, sevoflurane, methoxyflurane, nitrous oxide
what are the effects of inhaled anesthetics
myocardial and respiratory depression, N/V, decreased cerebral metabolic demand
list all of the intravenous anesthetics
barbituates, benzodiazepines, arylcyclohexamines (ketamine), opioids, propofol, etomidate
what’s the mechanism of action of ketamine
NMDA receptor blocker
what are the side effects of ketamine
cardiovascular stimulant, causes disorientation, hallucination and bad dreams as well as increased cerebral blood flow
name the ester and amine local anesthetics
ester- procaine, cocaine, tetracaine
amines- lidocane, mepivacane, bupivacane
how do local anesthetics work
bind and inhibit activated Na+ channels
what’s the order of sensory loss with local anesthetics
(1) pain, (2) temperature, (3) touch, (4) pressure
how does dantrolene work and what is it used for
blocks Ca2+ release from sarcoplasmic reticulum;
used for malignant hyperthermia
name the depolarizing and non-depolarizing neuromuscular blockers
depolarizing (strong AChR agonist)= succinylcholine
non-depolarizing (AChR antagonist)= tubocurarine, atracurium, mivacurium, pancuronium, vecuronium, rocuronium
name the five kinds of drugs that treat Parkinson’s
BALSA: bromocriptine (not really used in practice anymore) amantadine l-dopa with carbidopa selegiline antimuscarinic (benztropine)
how does selegiline work
inhibits MAO-B
what drugs are used to treat Alzheimer’s disease
memantine (NMDA receptor antagonist)
donepezil, rivastigmine, galantamine (AChE inhibitors)
what drugs are used to treat Huntington’s disease
tetrabenazine and reserpine (VMAT inhibitors)
haloperidol (dopamine receptor antagonist)
how does sumatriptan work and what is it used for
5HT agonist; blocks vasoactive peptide release in order to vasoconstrict
used for cluster headaches and acute migranes
what toxicity is associated with sumatriptan
coronary vasospasm, mild tingling
