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94 Cards in this Set
- Front
- Back
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- neurotransmitter
- mood (antidepressants effect it) - May be involved in anxiety - Pain regulation - learning & memory - Attention and arousal - Stress depletes it - Alpha & beta receptors - Drugs act on its synthesis, uptake, breakdown |
Norepinephrine
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- Neurotransmitter
- learning & memory - cognition - attention - wakefulness, arousal - degenerates in Alzheimer's - interaction with DA in striatum - schizophrenia - nicotinic & muscarinic receptors |
Acetylcholine
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- Neurotransmitter
- Parkinson's disease has too little of it - Schizophrenia has too much of it - Reward, reinforcement, addiction - Many drugs act through increase or blockade of it - 5 receptor subtypes |
Dopamine
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- Neurotransmitter
- Mood (depression tx w. reuptake inhibitors of it) - promotes sleep - anxiety - OCD - hunger or appetitie - perception (LSD) - Many receptor subytypes |
Serotonin
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- neurotransmitter
- inhibitory - modulates NMDA receptor |
Glycine
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- neurotransmitter
- major excitatory transmitter in CnS - Inotropic receptors (NMDA; AMPA) - Metabotropic receptors (excitatory postsynaptic; inhibits transmitter release presynaptically) - Memory & learning - excess activity may cause seizures - Neurotoxic in large amounts: stroke, ischemia |
Glutamate
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- Neurotransmitter
- Major inhibitory transmitter in CNS - Relieves anxiety - promtes sedation - BARbiturates, benzos, OH, all work at its A receptor - Baclofen works at its B receptor |
GABA
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- effects are supra additive (effects of 2 together are greater than sum of 2 alone)
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CNS depressants
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- Act on GABAa receptor to increase duration of GABA action (channel stays open longer)
- CNS depressant - disinhibit inhabtory neurons - induce anesthesia - anticonvulsants - head trauma SE: - Low margin of safety, over dose causes death - physical/psychological dependence (severe withrdrawal) - dangerous w/ alcohol CI: - porphyria - pulmonary insufficiency |
Barbiturates
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- Benzo
- longest half life (43 hours) - DOC: Epilepsy/seizures - used as a muscle relaxant - used in alcohol withdrawl |
Diazepam
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- Benzo
- used for epilepsy & seizures (absence & myoclonic siezures as well as infantie spasms) CI: - pregnancy category D |
Clonazepam
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- Benzo
- used in alcohol withdrawal |
Chlordiazepoxide
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- Benzo
- used to tx insomnia - Less interferrence with REM sleep than barbiturates - intermediate length of action so useful for sleep w/out hangover the next day |
Temazepam
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- Benzo
- used to treat insomnia - less interference w/ REM sleep than barbiturates - long acting so useful for early awakeners but may cause "hangover" the next day |
Flurazepam
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- intensify the action of GABA but don't open the channel themselves (so much safer than barbiturates)
- only act in presence of GABA - facilitate but don't increase maximum response - safe even in overdose - tolerance eventually develops - CYP3a metabolism - Elderly don't metabolize them as fast as younger patients - DOC for anxiety Uses: - anxiolytic - sedative-hypnotic - muscle relaxation - Alcohol or barbiturate withdrawl - anticonvulsant SE: - memory impairment in elderly & children - Respiratory depression (problem w/ sleep apnea) - can cause birth defects - can have severe withdrawal CI: - combined with alcohol can be lethal - pregnancy category D - children - sleep apnea |
Benzodiazepines
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- Benzo
- Used for Epilepsy & seizures - used in alcohol withdrawal - shorter half life |
Lorazepam
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- Benzo
- short surgical procdure drug used for sedation & anesthesia |
Midazolam
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- Benzo
- shorter half life - used for anxiety especially if there is also depression |
Alprozolam
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- Benzodiazepine antagonist
- reverse effect of benzodiazepines, Zolpidem, Azleplon, Exzopiclone - must be injected - Withdrawal/ seizures possible in Benzos, barbiturates, OH, epilepsy, TCA patients |
Flumazenil
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- Antihistamine
- Blocks H1 receptor - sedative effect - ok for occasional use |
Diphenhydramine
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- Bind to benzodiazepine receptor subtype BZ1
- Very rapid action "blackouts" - Few other effects - little effect on REM Sleep - Short term tx for insomnia - Short half life & duration of action SE: - Sleep walking, driving, eating - confusion & memory loss in elderly - Additive CNS depression w/ other drugs |
Zolpidem & Zaoleplon
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- sedative hypnotic "other"
- cheap and used in nursing homes - low margin of safety - gets converted to trichloroethanol and then works on the GABA receptor much like barbiturates do SE: - GI irritation - allergy - cardiac problems - liver dammage |
Chloral hydrate
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- Similar to Zolpidem but may bind to more BZ receptor types
- longer half life - approved for long term tx of insomnia - rebound insomnia or withdrawal possible after chronic use |
Escopiclone
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- partial agonist at 5-HT1a receptor
- Relieves anxiety - no sedation - some antidepressant effect through NeE, DA activity - Low addiction potential Uses: - anxiety - PMS - autism - Recovering addicts/alcoholics SE: - dizziness/headache - restlessness CI: - HTN in combo with MAOIs - don't combine w/ SSRIs |
Buspirone
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- Melatonin analogue used as sleep aid
- Resets slee wake cycle - No GABA effect - No REM effets - No addiction potential - Not controlled substance SE: - increase prolactin & decrease testosterone - can cause adrenocrotical insufficiency in high doses/long duration CI: - avoid in severe liver disease |
Ramelteon
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- Causes acetaldehyde buildup by inhibiting aldehyde dehydrogenase
- effects last 3-4 days - Can be dangerous SE: - flushing throbbing headache, nausea - confusion - hypotension |
Disulfiram
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- Benzos used in alcohol withdrawal
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Diazepam, Chlordiazepoxide, Lorazepam
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- Decreases likelihood of relapse
- decreases EtOH intake - no abuse potential - no liver toxicity - few other effects |
Acamprosate
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- CNS depressant (at high doses)
- Binds to GABAa receptor - inhibits NMDA receptors (amnesia) - Low doses (disinhibition) - Poor sleep quality - zero order kinetics - vasodilator (hypothermia) - mild diuretic - Uterine relaxation Drug interactions - acetaminophen (liver damage) - additive effect w/ other deppressants Toxicity: - seizures - decreased body temperature - hypoglycemia - hepatotoxic - cardiomyopathy - carcinogenicity CI: - pregnancy |
Alcohol
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- Opiod receptor antagonist
- blocks reward pathway - Reduces craving CI: - liver failure |
Naltrexone
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- to tx seizures from alcohol withdrawal
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Phenytoin
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- inhibit reuptake of NE & 5HT
- blocks muscarinic receptors - Antihistamine (makes you sleepy) - Alpha 1 blockade (postural hypotension, reflex tachycardia & inhibition of ejaculation) - No euphoria (low abuse potential) - takes 2-3 weeks to have affect - worse in elderly & children - tolerance develops to sedation - analgesia (spinal cord) Uses: - panic disorder (SSRIs more common) - Chronic pain (low dose) Fibromyalgia (los dose) SE: - wt gain - decreased seizure threshold - SIADH - Sedation - Cardiac arrhythmias (Torsades de pointes; give phenytoin) CI: - Benign prostatic hyperplasia (muscarinic receptor blockade) - cardiac disease (alpha 1 blockade) - don't combine w/ MAOI (severe CNS toxicity, serotonin syndrome) |
Tricyclic antidepressants
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- TCA
- 2ndry amine - least cardiac effect |
Nortriptyline
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- TCA
- used in migraine prophylaxis - Tertiary amine (more sedating/antcholinergic/5HT) |
Amytriptyline
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- TCA
- 2ndry amine - more cardiac effect |
Desipramine
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- TCA
- Tertiary amine (more sedating/antcholinergic/5HT)- more cardiac effect - used for enuresis (inhibits bed wetting) |
Imipramine
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- Monamine oxidase inhibitor
- used for depression which doesn't respond to other drugs (atypical depression) - irreversibly inhibit MAOa (breaks down NE & 5HT) & MAOb (breaks down DA) SE: - severe HTN crisis (from preventing the body from breaking down tyramine) - from tyramine in foods (red wine, beer, aged cheese) - similar HTN effects in combo w/ sympathomimetics (cold meds) - blocks both alpha 1 receptors & muscarinic receptors - in combo w/ dextromethrophan, TCAs or SSRIs causes: hyperpyrexia & or serotonin syndrome |
Phenelzine
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- SSRI
- useful for hot flashes |
Citalopram, Escitalopram
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- SSRI
- inhibits reuptake of 5HT - increases levels of TCAs, Benzos & antipsychitics by inhbiting CYP2D6 - DOC: depression - antidepressant effect takes 3-4 weeks - Inhibits NE uptake - long duration after drug continued (wait 5 weeks to switch to new anti depressant class) SE: - GI: nausea, loss of apetitie - Sexual disinterest/dysfunction - photosensitivity - SIADH |
Fluoxetine
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- inhibit reuptake of 5HT more selectively than TCAs
- few effects on other receptors |
SSRIs
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- SSRI
- approved for Social anxiety tx - DOC: OCD CI: - pregnancy |
Paroxetine
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-SNRI
- blocks reuptake of bothe 5HT & NE - useful in depression associated pain (fibromyalgia) CI: - liver disease |
Duoxetine
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- SNRI
- Blocks 5HT & NE reuptake - useful for hotflashes - like TCA w/out musc/alpha block - similar side effects to SSRIs - May increase blood pressu |
Venlafaxine
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- mechanism unkown
- "other" antidepressant - Do not combine with other antidepressants - photosensitivity |
St. John's Wort
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- "other" antidepressant
- significant sedation - used to tx insomnia & for pain management SE: - priapism |
Trazodone
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- inhibits DA reputake
- antidepressant "other" - may work where others don't - Few sexual side effects (combined w/ SSRIs to overcome sexual problems) - used to tx ADHD & alcoholism (decreases craving) SE: - Seizures possible at higher doses - Rash (discontinue) CI: - hx of seizures or head trauma |
Buproprion
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- "Other" antidepressant
- Alpha 2 selective antagonist - Used for depression w/ insomina - effects similar to TCAs w/out cardiac toxicity SE: - sedation - increased serum cholesterol - increased appetite |
Mirtazapine
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- first Antipsychotics to be developed "classical"
- higher affinity for D2 recpetor - control positive but not negative symptoms Uses: - schizophrenia - antiemetic - mania, hallucinations SE: - Extrapyramidal symptoms (akathisa, dystonia, parkinson's like, rigidity, tremor, etc) - itching - premature ejaculation - very sedating - Neuroleptic malignant syndrome |
Phenothiazines
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- Low potency on D2
- very anticholinergic - more likely to decrease siezure threshold SE: - Jaundice |
Chlorpromazine
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- Phenothiazine antipsychotic
- used as an antiemetic |
Prochlorperazine
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- Low potency phenothiazine
- very anticholnergic - less likely to have extrapyramidal symptoms - more likely to decrease siezure threshold SE: - retinal deposits |
Thioridazine
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- Potent D2 blockade
- no anticholinergic - injected in acute situations - used to tx Tourrette's - used to tx psychosis caused by PCP in the ER SE: - Extrapyramidal symptoms (akathisa, dystonia, parkinson's like, rigidity, tremor, etc) |
Haloperidol
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- new generation antipsychotic
- blocks D4 & 5HT recpetors - effective agasint both positive & negative symptoms - muscarinic, histamine alpha 1 receptor blockade SE: - sedation - wt gain - Agranulocytosis |
Clozapine
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- New generation antipsychotic drug
- blocks D2, D4 & 5HT receptors - controls both negative & positives symptoms - Similar to clozapine - used in bipolar disorder - doesn't caus agranulocytosis - Uses: - for Bipolar disorder/depression & mania w/ psychosis - first line against schizophrenia SE: - wt gain very common - sedation - Hyperglycemia (Type II DM) |
Olanzapine
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- New generation antipsychotic
- Dopamine system stabilizer - DA partial agonist, 5HT block - first line against schizophrenia SE: - May cause hyperglycemia (type II DM) - Esophageal motility problem |
Aripiprazole
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- New generation antipsychotic drug
- blocks D2, D4 & 5HT receptors - controls both negative & positives symptoms - DOC: psychosis, alzheimers - long acting preparation w/ once every 2 week dosing may improve compliance Uses: - Alzheimer's - first line against schizophrenia SE: - prolongs QT interval - Wt gain - May increase mortality if used in Alzhemier's disease |
Risperidone
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- block 5HT receptors
- improve negative symptoms - most also block D2 receptors - less if any extrapyramidal effects |
Newer antipsychotics
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- New generation antipsychotic drug
- blocks D2, D4 & 5HT receptors - controls both negative & positives symptoms - litle effect on prolactin Uses: - for Bipolar disorder/depression & mania w/ psychosis - antidepressant adjunct - first line against schizophrenia SE: - wt gain - sedation |
Quetiapine
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- New generation antipsychotic drug
- blocks D2, D4 & 5HT receptors - controls both negative & positives symptoms - used in acute mania & Tourette's SE: - Prolongs QT interval Seizures possible - Sedating - Hyperprolactinemia |
Ziprasidone
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- mechanism unkown
- First choice drug for mood stabalizing - very toxic in overdose - slow onset of action - excreted by the kidneys - Lithium competes w/ Na for reabsorption in kidney so if Na is low lithium toxicity can result - safe in pregnancy if necessary SE: - tremor - wt gain - edema - rashes - thyroid disorder - diabetes insipidus (tx w/ amiloride) CI: - in combo w/ thiazide diuretics (they decrease Na reabsorption) - in combo w/ NSAIDs inhibit PG synthesis so decrease Li clearance & lead to toxicity |
Lithium as a mood stabalizer
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- Mood stabalizer
- effective in non responders to Li or in combo w/ it - DOC: sequres partial, tonic, cloinc SE: - Stevens Johnson syndrome CI: - pregnancy |
Carbamazepine
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- Mood stabalizer
- used in migraine prophylaxis - inactivation of Na channels - potentiates GABA receptors - Inhibits glutamate receptor - causes wt loss Uses: - partial seizures - Generalized tonic clonic seizures - Mygrain prophylaxis - wt loss - alcoholism SE: - acute myopia/glaucoma - pregnancy category C so use with caution only if neessary |
Topiramate
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- Anticonvulsant w/ antimanic effects
- used in migraine prophylaxis - used as mood stabalizer - used in those who don't respond to Li, or in combo w/ Li SE: - Liver toxicity - wt gain CI: - pregnancy |
Valproic acid
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- inactvates NA channels
- Anticonvulsant Uses: - often used as an add on but sometimes by itself for partial seizures - biplar disorder SE: - Stevens johnson syndrome (1 of the big 4 for SJS) - pregnancy category C |
Lamotrigine
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- Anticonvulsant
-Class 1b sodium channel blocker - Blocks inactivated Na channels to shorten action potentials - decrease effective refractory period w/ no change in QRS or QT - prolongs Na channel inactivation - Induces P450 - dose dependent elimination - oral/IV - DOC for tonic clonic seizure - not effective for absence seizures - Fosphenytone is soluble progdrug for injection - 1st order elimination at low doses but 0 order at therapeutic & higher doses Used to Tx: - partial & tonic-clonic seizures - digoxin induced ventricular arrythmias SE: - gingival hyperplasia - hirsutism - nystagmus - double vision - Stevens johnson syndrome (1 of the big 4 for SJS) - diplopia & ataxia CI: - pregnancy category D |
Phenytoin
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- GABA agonist
- Anticonvulsant |
Diazepam
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- typically work on either Na or Ca channels or both
- Monotherapy is best - not good for pregnancy and can result in congenital heart defects & neural tube defects |
Anticonvulsants
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- Barbiturate
- prolongs opening of chloride channel at GABAa receptor - Alters Na & Ca conductance at high concentrations - DOC: seizures tonic clonic, partial, preganancy SE: - Stevens Johnson syndrome CI: - porphyria - pregnancy category D |
Phenobarbital
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- ca channels
- DOC: absence seizures - valproic acid inhibits its metabolism & increases its half life SE: - Stevens johnson syndrome (1 of the big 4 for SJS) - hiccup - euphoria - pregnancy category C |
Ethosuximide
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- anticonvulsant adjunct for partial & generalized tonic-clonic seizures
- also used for neuopathic pain (main use) - low efficacy long term as mood stabalizer SE: - sedation - wt gain - pregnancy category C |
Gabapentin
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- Readily crosses BBB and is converted to dopamine in the neuron
- DOC: to tx parkinson's - effectiveness goes down over time CI: - psychosis - closed angle glaucoma - Malignant melanoma |
Levodopa
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- inhibits dopa decarboxylase & doesn't cross BBB
- inhibits conversion of Levodopa to DA in the periphery but not in the CNS (decreases peripheral side effects of Levodopa) |
Carbidopa
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- MAO inhibitor
- inhibits MAOb but no MAOa - reduces striatal metabolsim of DA - doesn't effect peripheral metabolism of DA - used in combo w/ Levodopa SE: - Insomnia - Svere HTN in combo w/ other MAOIs - Serotonin syndrome if combined w/ TCAs or SSRIs - Don't combine w/ meperidine |
Selegiline & Rasagiline
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- COMT inhibitor in CNS & periphery
- inhibits DA metabolism; prlongs DA action - Stalevo: combo of Levodopa/carvidopa/entacopone SE: - orange color in urine |
Tolcapone
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- COMT inhibitors
- inhibits DA metabolism; prlongs DA action - inhibits COMT in periphery only SE: - orange color in urine - death from hepatic failure |
Entacapone
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- Stimulates DA receptors
- can cause hot red feet |
Bromocriptine
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- used for rescue of off periods in patients on optomized levodopa therapy
SE: - nausea (take with antiemetic) |
Apomorphine
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- Relatively pure DA D2 agonist
- DOC for restless leg syndrome |
Ropinirole
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- Dopamine receptor agonist
- FDA warning on possible heart failure |
Pramipexole
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- antiviral used for influenza
- used to tx early or mild cases of parkinson's disease (especially for tremors) SE: - toxic psychosis & convulsion may occur with overdose |
Amantadine
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- restore striatal DA/ACH balance
- used in early & late stages SE: - constipation - urinary retention - blurred vision - sedation - confusion |
Anticholinergics in parkinsons tx
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- NMDA receptor antagonist
- used in late/severe stages of disease CI: - in combo w/ meperidine |
Memantine
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- Cholinesterase inhibitor
- increase the amount of ACH in nerve terminal - DOC for alzheimers - once a day dosing |
Donepezil
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- Cholinesterase inhibitor
- increase ACH in nerve terminal SE: - GI nausea, vomiting, diarrhea, stomach cramps |
Rivastigmine & Galantamine
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- Agonist at GABAb receptors
- opens K shannels (hyerpolarization) - reduces pain by inhibiting substance P release - intrathecal administration possible SE: - increased seizure activity - respiratory depression can occur w/ intrathecal admin |
Baclofen
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-Muscle relaxing sedative
- Sedative at brain stem - used for acute muscle spasm antimuscarinic SE: - sedation/confusion common - possible hallucinations |
Cyclbenzaprine
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-Muscle relaxing sedative
- Sedative at brain stem - used for acute muscle spasm - may alter perception of pain - chronic use induces hepatic enzymes - Now a popular drug of abuse |
Carisoprodol
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- inhibits ACH release
- small amounts injected locally to control muscle spasms - toxic in large amounts |
Botulinum Toxin
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- Alpha 2 receptor agonist
- inhibits pain transmission - used for chronic & acute muscle spasms SE: - sedation - hypotension - dry mouth - weakness, falls in elderly |
Tizanidine
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- interferes w/ excitation-contraction coupling in muscle fiber
- muscle relaxant - decreases Ca relase from sarcoplasmic reticulum - Skeletal muschel affected more than cardiac or smooth muscle Uses: - malignant hyperthermia - neuroleptic malignant syndrome |
Dantrolene
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- CNS stimulant
- decreases hyperactivity & improves attention |
Methyphenidate
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- CNS stimulant
- blocks adeonisine receptors - inhibits PDE to increase cAMP - Constriction of cerebral blood vessels ( useful in headache |
Caffeine
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- CNS stimulant
- Sympathomimetic that mimics epinephrine - Sterotypic behavior - paranoia - delusions - hallucinations - psychosis - high abuse potential - changes "setpoint" in brain (more drug neeed just to feel ok |
Amphetamines
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- CNS stimulant
- inhibits reuptake of NE - little addiction potential |
Atomoxetine
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