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Neuro Pharm
Keck Neuro pharm
118
Pharmacology
Graduate
04/23/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Pilocarpine
Definition
Muscarinic agonist used for rx of closed angle glaucoma bc causes miosis
Term
Atropine
Definition
Muscarinic blocker, used for dilating pupils for eye exams
Term
Physostigmine
Definition
ChE inhibitor used for closed angle glaucoma bc of miosis
Tertiary amine (preferable bc easily crosses membranes)
Term
Dorzolamide
Definition
carbonic anhydrase inhibitor that is used for open angle glaucoma bc decreases aqueous formation
Term
Timolol
Definition
Beta blocker (B1=B2) that inhibits epinephrine release which reduces aqueous; may cause asthma attacks
Term
Betaxolol
Definition
Beta blocker (B1 > B2) --> inhibits E release --> reduces aqueous; safer for asthmatics than timolol
Term
Aproclonidine
Definition
Alpha 2 agonst that decreases aqueous & increases uveoscleral aqueous outflow
Term
Latanoprost
Definition
PGE2 analog that increases uveoscleral output. Side effects are longer eyelashes & discolored iris
Term
p-chlorophenylalanine
Definition
Blocks tryptophan hydroxylase
Term
Reserpine
Definition
Blocks VMAT --> Depletes 5HT, NE (used to treat depression)
Term
MDMA
Definition
indirect agonist that releases 5HT --> acts on all receptors
Term
Barbiturates for sleep
Definition
used for cataplexy (narcolepsy) but build up tolerance & decreases delta sleep
Term
Amitryptyline for sleep
Definition
antidepressant - sedative that helps w sleep in already depressed pts (downside = hypotension)
Term
Trazodone
Definition
antidepressant - sedative that helps w sleep in already depressed pts (downside = hypotension)
Term
Doxepin
Definition
antidepressant - sedative that helps w sleep in already depressed pts (downside = hypotension)
Term
Antihistamines for sleep
Definition
sedative but has anticholinergic side effects
Term
Flurazepam- for sleep
Definition
benzodiazepine w/ little-no REM suppression or rebound, long acting
Term
Temazepam - for sleep
Definition
benzodiazepine w/ little-no REM suppression; intermediate acting but slow onset & possible rebound insomnia
Term
Triazolam - for sleep
Definition
shortest acting benzodiazepine - has REM suppression, anterograde amnesia, rebound insomnia
Term
Zolpidem
Definition
BZD1 receptor - safer than benzos, doesn't affect sleep stages, has a quick onset
Side effects: drowsiness, headache, N/D/Dizziness
Term
Zaleplon
Definition
BZD1 receptor - safer than benzos, doesn't affect sleep stages, has a quick onset & ultra-short acting (t1/2 = 1 hr) - good for sleep initiation problems
Side effects: memory problems
Term
Eszopiclone
Definition
BZD1 receptor - safer than benzos, doesn't affect sleep stages, has a quick onset, intermed acting (t1/2 = 6 hr); efficacy >6 mos
Term
Melatonin receptor agonists
Definition
short acting, reduce sleep latency, and work by acting thru suprachiasmatic nucleus; but inconsistent results / no regulation
Term
Phenytoin
Definition
anti-seizure for complex partial seizures
Term
Carbamazepine
Definition
anti-seizure for complex partial seizures
Term
Valproate
Definition
Anti-convulsant / anti-seizure for absence generalized seizures
Term
Amitryptyline
Definition
TCA; inhibits presynaptic NT reuptake (NE, 5HT, DA)
Effective & inexpensive
AE's: sedation (H1 blocker), orthostatic hypotension, dizziness (alpha-1 blockade), dry mouth & constipation (cholinergic blockade)
Term
Fluoxetine
Definition
SSRI; inhibits presynaptic 5HT reuptake
Approved for >8 yrs old
AE's: N/D, sexual side effects, insomnia, headache
Term
Phenelzine
Definition
MAOI; inhibits breakdown of NT
Effective & cheap
AE's: dizziness, orthostatic hypotension (a1 blockade), insomnia; do not mix w tyramine (red wine, cheese); fatal if combined w SSRI
Term
Buprporion
Definition
aka wellbutrin; dopamine reuptake inhibition; used for depression
No weight gain or sexual side effects
AE's: insomnia, GI, lower seizure threshold
Term
Mirtazapine
Definition
aka Remeron; 5HT2 antagonist --> increases 5HT + a2 antagonist --> increase NE; used for depression
AE's: weight gain, sedation
Term
Litihum
Definition
NT stabilizer; inhibits NE & DA + enhances 5HT used for tx of bipolar;
AE's: intentional tremor, weight gain, polyuria
Takes 1-3 weeks for onset and has interactions w/ caffeine & iburpofen
Term
Valproate
Definition
Anticonvulsant also used for bipolar (mixed mania/rapid cycling); increasese GABA
quick onset
AE's: weight gain, sedation
Term
LSD
Definition
5HT2a partial agonist
Term
Benzodiazepine
Definition
GABA-A agonist that increases the frequency of Cl- channel opening
Anxiolytic - used for GAD, situational anxiety, panic disorder, general anesthesia
AE's: CNS depression, impaired judgment, anterograde amnesia, respiratory depression
Term
Pentobarbital
Definition
Barbiturate; GABA-A agonist
Term
Picrotoxin
Definition
GABA-A & glycine inhibitor (non-competitive);
Toxicity = tonic clonic seizures
used for barbiturate poisoning
Term
Bicuculline
Definition
Convulsant; GABA-A antagonist
Term
Baclofen
Definition
GABA-B agonist
Term
gamma hydroxybutyrate (GHB)
Definition
breakdown product of GABA that causes coma, seizures, vomiting, depression, amnesia
Term
Strychnine
Definition
Glycine receptor antagonist; convulsant
Does NOT act on GABA!
Treat OD w/ CNS depressant (diazepam)
Term
Cocaine
Definition
Indirect acting sympathomimetic
Blocks NET (uptake 1) --> increases NE & DA
Sx = mydriasis, tachycardia, htn, hyperthermia (from vasoconstriction)
Can be used in nasal surgery (good vasoconstriction)
Term
Pseudoephedrine
Definition
Indirect acting sympathomimetic
Blocks NET (uptake 1) + stimulates NE release --> increases NE
Sx = arousal, euphoria, vasoconstriction (reduces congestion), tachycardia (B1 > reflex bradycardia)
Term
Tyramine
Definition
Found in red wine & cheese; displaces NE from synaptic vesicles --> increases NE release
Tyramine + amphetamine = depletion of NE
Tyramine + MAOI = way too much NE
Term
Fenoldopam
Definition
D1 receptor agonist; used to treat hypertension by stimulating vasodilation
Term
Epinephrine - low dose
Definition
a1, B1, B2 agonis; B2 > a1 --> decrease diastolic bp (but no change in overall BP), HR increases (B1 - no reflex bc no BP change)
Term
phenylephrine
Definition
alpha1 agonist; used for nasal decongestion, hypotension. Side effect = mydriasis
Term
Epinephrine - high dose
Definition
a1, B1, B2 agonist; a1 > B2 --> increase diastolic BP
Term
Norepinephrine
Definition
a1, B1 agonist --> increase BP; HR decreases (reflex)
Term
Isoproterenol
Definition
B1 = B2; decrease diastolic BP (B2), increase systolic = (very small decrease in overall BP); HR increases (B1); used for Rx of arrhythmias
Term
Clonidine
Definition
a2 agonist --> decreases NE; used for nicotine addiction, opiate addiction, benzo addiction (reduces sympathetic side effects of withdrawal)
Term
Dobutamide
Definition
B1 agonist - increases HR
Term
Albuterol
Definition
B2 agonist - bronchodilation + vasodilation (decrease in BP)
Term
Prazosin
Definition
a1 blocker - used to treat BPH; side effect = hypotension
Term
Phenoxybenzamine
Definition
a1 blocker (some a2) - used to treat pheochromocytoma (adrenal hyperplasia = increase E release)
Term
Propanalol
Definition
B1 = B2 blocker; decreases BP (but not good for asthmatics); NO reflex tachycardia
Term
Metoprolol
Definition
B1 selective blocker; decreases BP + NO reflex tachycardia
Term
Labetolol
Definition
a1, B1, B2 blocker; decreases BP; NO reflex tachycardia
Term
Phentolamine
Definition
a1, a2 blocker; used to treat erectile dysfunction --> vasodilation in penis
Term
Ethanol
Definition
GABA-A agonist (inhibits adenosine reuptake); causes paradoxical excitation (via disinhibition); used for trigeminal neuralgia, poison ivy, methanol poisoning; AE's: ataxia, resp depression, diuresis, gastric acid secrtion
Term
Barbiturates
Definition
Prolongs GABA Cl- channel opening; used for mild sedation, anticonvulsant, anxiolytic, sleep
Term
Diphenhydramine
Definition
Blocks tuberomammillary H projections; blocks H1 --> mild sedation
Term
Ramelteon / melatonin
Definition
acts on receptors in suprachiasmatic nucleus --> cause mild sedation; used for rx of insomnia
Term
Disulfiram
Definition
Blocks acetaldehyde dehydrogenase (enzyme in breakdown of alcohol); used for alcohol rehab bc causes really bad hangover effects if any alcohol is had
Term
Buspirone
Definition
5HT1a autoceptor agonist / 5HT2/7 blockade - after 4-6 wks downregulates autoceptor (increase 5HT); anxiolytic & mild sedative; does not interact w/ alcohol
For Rx of GAD (equally effective to benzos)
Term
Clozapine
Definition
5HT2/7 blockade --> increases slow wave sleep
Term
Clonazepam
Definition
Tx of personality disorder; calming & anxiety reduction
Benzo
Term
Diazepam
Definition
Benzo
used as an anticonvulsant
Term
Chlorodiazepoxide
Definition
Benzo w/ longer half-life
Term
Alprazolam
Definition
Benzo
Used for personality disorder tx
Term
Venlafaxine
Definition
SSRI + SNRI; inhibits reuptake + downregulates
Term
Flumazenil
Definition
Used for treatment of benzo overdose
Term
Pentylenetetrazole (metrazole)
Definition
GABA receptor antagonist --> convulsant
Used to activate EEG for diagnosing siezure d/o
Term
Xanthines (Caffeine, theophylline, theobromine)
Definition
Blockade of adenosine A1 & A2 recptors --> increase Ca++ --> increase cAMP
Clinical use = prolonged episodes of apnea in preemies
Effect: alert, nervous, convulsions (v high doses); bronchial muscle relaxation, diuretic, increases HR
Toxicity = PVCs, delirium, emesis
Term
Theophylline
Definition
Xanthine, clinical use = bronchodilation
Term
Benzedrine
Definition
racemic amphetamine; stimulates NE (&DA) release and blocks reuptake
Clinical use: narcolepsy, ADHD, obesity
Effects: sympathomimetic, increase BP & reflex bradycardia
Term
Dexedrine
Definition
D isomer amphetamine
stimulates NE (&DA) release and blocks reuptake
Clinical use: narcolepsy, ADHD, obesity
Effects: sympathomimetic, increase BP & reflex bradycardia
Term
Metamphetamine
Definition
Amphetamine but with fewer peripheral effects;
stimulates NE (&DA) release and blocks reuptake
Clinical use: narcolepsy, ADHD, obesity
Effects: sympathomimetic, increase BP & reflex bradycardia
Term
Methylphenidate
Definition
aka Ritalin; sympathomimetic used to treat ADHD
Term
Modafinil
Definition
sympathomimetic used as an alertness-enhancing drug
Term
nicotine
Definition
Binds nicotinic receptors, increases DA in nuc accumbens
Used in early alzheimer's
Effects = alertness, euphoria, muscle relaxation, appetite reduction, increased HR & BP, GI motility
Treat addictions w Clonidine, buproprion, varenicline
Term
Doxapram
Definition
Carotid K+ channel blocker --> increased DA release
Effects = respiratory stimulation
Use = COPD, anesthesia recovery
Treat OD w/ short-acting barbiturate
Term
Kainic acid
Definition
binds to kainate receptor (more so than glutamate)
Term
PCP
Definition
competes with Mg2+ on NMDA (glutamate) receptor --> blocks receptor --> hallucinations, delusions, cognitive deficits
Term
Anandamides
Definition
endogenous cannabinoids - act on CB1 receptor in CNS & CB2 in periphery
Effects = anxiety, insomnia, depression, sperm morphology, birth defects, impaired attention
Term
Beta endorphins
Definition
Endogenous opioids made in hypothalamus & pituitary (POMC); bind to mu & Delta
Term
Enkephalins
Definition
Endogenous opioids found in CNS, adrenal, enterics; synthesized by preproenkephalin
bind to mu & delta
Term
Dynorphins
Definition
Endogenous opioid - in CNS & spinal cord especially; synthesized by preprodynorphin
Kappa (and weak mu) agonist
Term
Morphine
Definition
Opioid agonist used for severe pain
Given parenterally
long duration
Term
Codeine
Definition
Orally effective opioid, but less potent than morphine
Good antitussive
synergystic effect w/ aspirin
Term
Heroin
Definition
opioid; Crosses BBB --> strong CNS effect
High abuse potential
Term
Methadone
Definition
opioid
oral efficacy + long duration (not as much withdrawal)
used for treating opioid addictions
Term
Meperidine
Definition
Opioid (demerol) : less potent than morphine; orally effective.. But NO antitussive, constipation, miosis
Good for acute pain / labor
Term
Fentanyl
Definition
very potent opioid; short duration
used for anesthesia
no histamine release
Term
Propoxyphene
Definition
opioid (darvon) - similar to codeine but lower efficacy (banned by FDA)
Term
Butorphanol
Definition
mixed opioid agonst/antagonist
more potent than morphine - parenteral or nasal spray
Psychotomimetic side effects
Term
Pentazocine
Definition
mixed opioid agonst/antagonist
less potent than morphine
can cause increase in BP (but has less respiratory depression)
Term
Buprenorphine
Definition
mixed opioid agonist/antagonist that is long acting, with slow dissociation from mu receptor --> decrease efficacy + long acting = very effective in treating opiate dependence
Term
Loperamide
Definition
Opioid does not cross BBB; used as a anti-diarrheal
Term
Dextromethropan
Definition
Opioid, but also blocks NMDA receptor --> good antitussive but no analgesia or respiratory depressoin
Term
Naloxone
Definition
opioid antagonist
short half life, parenteral
Good for opiate overdose (cheapest)
Term
Naltrexone
Definition
opioid antagonist
long half life + oral bioavailability = good for treating opiate addictions (in highly motivated ppl); also used to treat alcohol addiction
Term
Nalmafene
Definition
opioid antagonist
longer half-life than naloxone, but still parenterally given (probably preferable to naloxone in treating heroin overdose, but much more $$$)
Term
Chloropromazine
Definition
typical, low-potency antipsychotic
Blocks D2-4, 5HT2A, alpha1, M, H1
Used for acute psychosis, psychosis w/ positive symptoms
side effects = anticholindergic, neuroleptic malignant syndrome (but low EPS)
Term
Thioridazine
Definition
typical, low-potency antipsychotic
Blocks D2
side effects = prlonged QT interval
Term
Fluphenazine
Definition
typical, hi-potency antipsychotic
D2-4 block
Acute antipsychotic
side effects = EPS, lactation, sedation, Tardive
Term
Haloperidol
Definition
typical, hi-potency antipsychotic
D2-4 block
Acute antipsychotic
side effects = EPS, lactation, sedation, Tardive
Term
Clozapine
Definition
Atypical antipsychotic
D4 block (also 5HT2A, alpha1, M, H1)
side effects = seizures, paradoxical salivation, anticholinergic effects, sedation
Term
Olazapine
Definition
Atypical antipsychotic
5HT2A > D2-D4, a1, H1, M block
Used for negaive symptoms, bipolar mania
side effects = weight gain, diabetes, anticholinergic; don't use in elderly
Term
Risperidone
Definition
Atypical antipsychotic
5HT2A > D2-D4, a1, H1, M block
Best for elderly
side effects = postural hypotension, weight gain, agitation
Term
Pargyline
Definition
Inhibits MAO activity
Term
Glatiramer acetate
Definition
Used for MS treatment --> downregulates TH1, upregulate Tregs
Reduces relapse > interferons
Term
Interferon Beta 1a (Avonex, REBIF)
Definition
For MS treatment
Reduces relapse rate, development of new lesions, lesion growth
Side effects = psych, seizures, hepatitis, cardiomyopathy, autoimmune
30% develop neutralizing antibody
Term
Interferon Beta 1b (Betaseron)
Definition
For MS treatment
similar to beta 1a, but questionalbe duration & significance of benefit
May develop neutralizing antibodies
Term
Mitoxantrone (Novantrone)
Definition
For MS treatment
Reduces attack rate, slows disease progression
IV only, can cause local tissue damage, potentially fatal CHF may occur - very cardiotoxic
Term
Tysabri / Natalizumab
Definition
MAB therapy for MS
Effective in reducing attacks & new MRI lesions (no long-term data)
1/300 risk of PML if + for JCV
Term
Gilenya (fingolimod)
Definition
Sphingosine 1-phosphate receptor modulator, treatment for MS
First line oral therapy, produces lymphopenia in the brain?
Side effects = many
Term
Glucocorticoids
Definition
Short-term benefit for MS treatment
Good rx for acute attacks by restoring BBB
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