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143 Cards in this Set
- Front
- Back
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Sumatriptan
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5-HT 1B/1D agonist
- inhibits trigeminal nerve activation - prevents vasoactive peptide release - induces vasoconstriction - Acute Migraine + Cluster Headache - toxicity: coronary vasospasm & tingling |
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Haloperidol
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Dopamine antagonist
- Huntington's |
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Tetrabenazine
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inhibit VMAT
- limit dopamine packaging & release - Huntington's |
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Reserpine
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inhibit VMAT
- limit dopamine packaging & release - Huntington's |
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Donepezil
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inhibits AChE
- Alzheimer's - toxicity: nausea, dizziness, insomnia |
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Galantamine
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inhibits AChE
- Alzheimer's - toxicity: nausea, dizziness, insomnia |
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Rivastigmine
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inhibits ACheE
- Alzheimer's - toxicity: nausea, dizziness, insomnia |
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Memantine
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NMDA receptor antagonist
- Alzheimer's - toxicity: dizziness, nausea & hallucinations |
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Selegiline
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MAO-B inhibitor = increases Dopamine
- Parkinson's |
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actions of L-Dopa in Parkinson's
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crosses BBB and converted to dopamine by dopa decarboxylase
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action of Carbidopa in Parkinson's
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peripheral decarboxylase inhibitor
- increases bioavailability of L-dopa in brain |
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side effect of L-dopa & Carbidopa
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- Arrhythmias: increased peripheral conversion of catecholamines
- Dyskinesia: following administration - Akinesia: btw doses |
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what effect does Vit.B6 have on L-dopa?
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increases peripheral metabolism of L-dopa
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which Parkinson's drug improves tremor and rigidity?
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Benztropine
- antimuscarinic - little effect on bradykinesia |
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drug for Essential or Familial Tremors
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Propranolol
- beta-blocker |
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Entacapone, Tolcapone
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COMT inhibitors
- prevent L-dopa degradation - Parkinson's |
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Amantadine
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increases Dopamine
- Parkinson's - toxicity: ataxia |
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Pramipexole
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Dopamine agonist
- Parkinson's |
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Ropinirole
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Dopamine agonist
- Parkinson's |
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Dantrolene
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prevents Ca2+ release from SR
- Malignant Hyperthermia - Neuroleptic Malignant Syndrome |
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Succinylcholine
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NMJ blocking agent
- ACh receptor agonist - produces sustained depolarization & prevents muscle contraction |
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Phase 1 of NMJ blockade
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prolonged depolarization
- no antidote - block potentiated by cholinesterase inhibitors |
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Phase 2 of NMJ blockade
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depolarized but blocked
- ACh receptors are available, but desensitized - antidote = cholinesterase inhibitors (Neostigmine) |
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toxicity of depolarizing NMJ blockers
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hypercalcemia, hyperkalemia (arrhythmias) & malignant hyperthermia
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local anesthetics - esters
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Procaine, Cocaine, Tetracaine
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local anesthetics - amides
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Lidocaine, Mepivacaine, Bupivacaine
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action of local anesthetics
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- block Na+ channels by binding to specific receptors on inner portion of channel
- preferentially bind to activated Na+ channels |
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action of tertiary amines in local anesthesia
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penetrate membrane in unchanged form, then bind to ion channels as charged forms
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function of local anesthetics plus vasoconstrictors like Epinephrine
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- decrease bleeding
- increase anesthesia - decrease systemic concentration |
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order of nerve blockade
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smaller diameter fibers > larger diameter fibers
myelinated fibers > unmyelinated fibers ** size factor predominates |
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order of loss in local anesthetics
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pain, temperature, touch, pressure
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Bupivacaine toxicity (local anesthetic)
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severe cardiovascular toxicity
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Propofol
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potentiates GABA-a
- sedation in ICU - rapid anesthesia induction - short procedures |
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Ketamine
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PCP analog - blocks NMDA receptors
- IV anesthetic - cardiovascular stimulant - toxicity: disorientation, hallucinations & bad dreams, increased cerebral blood flow |
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most common drug used for endoscopy
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Midazolam
- severe post-op respiratory depression - decreased BP - amnesia |
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Thiopental
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barbiturate
- high potency, high lipid solubility, rapid entry into brain - induction of anesthesia & short surgical procedures - decreased cerebral blood flow |
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how is effect of Thiopental terminated?
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rapid redistribution into tissue and fat
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inhaled anesthetics
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Halothane, Enflurance, Isoflurance, Sevoflurane, Methoxyflurane, NO
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effect of inhaled anesthetics
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myocardial depression
respiratory depression nausea, emesis increase cerebral blood flow |
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Halothane toxicity (inhaled anesthetic)
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hepatotoxicity = hepatic necrosis
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Methoxyflurane toxicity (inhaled anesthetic)
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nephrotoxicity
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Enflurane toxicity (inhaled anesthetic)
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proconvulsant
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Malignant Hyperthermia
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caused by inhaled anesthetics (Halothane) except NO
- life-threatening - inherited susceptibility |
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drugs with DECREASED solubility
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rapid induction and recovery times
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drugs with INCREASED solubility
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increased potency = decreased MAC
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definition of MAC
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Minimal Alveolar Concentration at which 50% of population is anesthetized
- varies with age |
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solubility of Halothane
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increased lipid and blood solubility
- high potency and slow induction |
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solubility of Nitrous Oxide
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decreased lipid and blood solubility
- fast induction and low potency |
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HIGH blood/gas partition coefficient
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- more soluble in blood
- slower onset of action - slower equilibrium with brain |
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Zolpidem
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BZ1 subtype of GABA receptor
- insomnia - toxicity: ataxia, confusion & headache |
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Zaleplon
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BZ1 subtype of GABA receptor
- insomnia - toxicity: ataxia, confusion & headache |
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Eszopiclone
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BZ1 subtype of GABA receptor
- insomnia - toxicity: ataxia, confusion & headache |
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Benzodiazepines overdose tx.
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Flumazenil = GABA competitive antagonist
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drugs for Alcohol Withdrawal
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Diazepam (first) or Chlordiazepoxide
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Benzodiazepines not metabolized by liver
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Lorazepam & Diazepam
- good for Liver Disease |
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side effects of Benzodiazepines
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- dependence
- additive CNA depression effects with alcohol - less respiratory depression & coma with Barbiturates |
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drug for Sleepwalking
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Benzodiazepines
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drug for Night Terrors
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Benzodiazepines
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mechanism of Benzodiazepines
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increase FREQUENCY (intensity) of CI- channel opening = facilitate GABA-a
- decrease REM sleep |
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short acting Benzodiazepines
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Triazolam, Oxazepam & Midazolam
- higher addictive potential |
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mechanism of Barbiturates
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increase DURATION of CI- channel opening = facilitate GABA-a
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side effects of Barbiturates
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- respiratory & cardiovascular depression
- CNS depression - dependence - induce P450 |
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Barbiturates overdose tx.
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supportive - assist respiration and maintain BP
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Phenytoin
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blocks Na+ channels; inhibits glutamate release
toxicity: - nystagmus, diplopia - ataxia - SLE-like syndrome - gingival hyperplasia - hirsutism - megaloblastic anemia - lymphadenopathy |
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1st line prophylaxis for Status Epilepticus
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Phenytoin
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epileptic drug that causes gingival hyperplasia
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Phenytoin
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epileptic drug that causes fetal hydantoin syndrome
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Phenytoin
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epileptic drug that causes lymphadenopathy
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Phenytoin
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epileptic drug that causes hirsutism
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Phenytoin
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epileptic drug that cause mental dulling & kidney stones
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Topiramate
- blocks Na+ channels - increased GABA action |
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Topiramate
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blocks Na+ channels & increases GABA action
- migraine prevention |
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Gabapentin
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GABA analog; inhibits activated Ca2+ channels
- peripheral neuropathy, postherpetic neuralgia, migraine prophylaxis & bipolar disorder |
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epileptic drug used for migraine prophylaxis
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Gabapentin
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epileptic drug used for peripheral neuropathy
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Gabapentin
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Gabapentin toxicity
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sedation & ataxia
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Lamotrigine
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blocks Na+ channels
- epilepsy - toxicity: Stevens-Johnson Syndrome |
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1st line treatment for Absence Epilepsy
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Valproic Acid
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Valproic acid
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increases Na+ channel inactivation & increases GABA
- toxicity: fatal hepatotoxicity, spina bifida, GI distress, tremor, weight gain |
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epileptic drug that causes fatal hepatotoxicity
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Valproic Acid
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epileptic drug that causes neural tube defects in fetus
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Valproic Acid
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epileptic drug used for Absence seizures that blocks thalamic T-type Ca2+ channels
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Ethosuzimide
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Ethosuzimide toxicity
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GI distress, fatigue, headache & urticaria
Stevens-Johnson Syndrome |
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1st line drug for Trigeminal Neuralgia (sharp pain around jaw)
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Carbamazepine
- increases Na+ channel inactivation |
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epileptic drug that causes agranulocytosis & aplastic anemia
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Carbamazepine
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Carbamazepine toxicity
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diplopia, ataxia, liver toxicity, SIADH, Stevens-Johnson Syndrome, aplastic anemia & agranulocytosis
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epileptic drugs that induce P450
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Phenytoin
Carbamazepine Phenobarbital |
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1st line treatment for seizures of Eclampsia
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MgSO4
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epileptic drugs used for seizures of Eclampsia
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Diazepam or Lorazepam
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1st line treatment for acute status epilepticus
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Diazepam or Lorazepam
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Tiagabine
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epileptic drug that inhibits GABA reuptake
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Vigabatrin
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epileptic drug that irreversible inhibits GABA transaminase = increases GABA
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drug used for chronic pain
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Tramadol
- weak opioid - inhibits Serotonin & NE reuptake |
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anti epileptic drug converted to Phenobarbital & PEMA
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Primidone
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mu-opioid receptor PARTIAL agonist and kappa-opioid agonist
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Butorphanol
- used for severe pain |
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partial mu-opioid agonist that can cause withdrawal symptoms
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Pentazocine
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Opioid overdose tx.
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Naloxone or Naltrexone (greatest affinity for mu receptors)
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tolerance to Opioid analgesics does not develop to what?
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miosis and constipation
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drug used for maintenance programs for Opioid addicts
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Methadone
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Opioid used for cough suppression
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Dextromethorphan
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Opioids used for diarrhea
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Loperamide & Diphenoxylate
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Opioid mechanism of action
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mu= Morphine
delta = Enkephalin kappa = Dynorphin - open K+ channels & close Ca2+ channels |
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clinical use for Opioids
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pain, cough suppression, diarrhea, acute pulmonary edema
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Latanoprost (PFG-2alpha)
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increases outflow of aqueous humor
- treat glaucoma - toxicity: darkens color of iris |
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Acetazolamide in glaucoma
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- angle closure glaucoma
- decreases aqueous humor synthesis via inhibition of CA |
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Beta-blockers for Glaucoma
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Timolol, Betaxolol, Carteolol
- decrease aqueous humor synthesis = via ciliary epithelium |
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Brimonidine (alpha-2 agonist)
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decreases aqueous humor synthesis
- Glaucoma |
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drug for glaucoma emergencies
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Pilocarpine
- opens meshwork into canal of Schlemm - indirect cholinomimetic |
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direct cholinomimetics for glaucoma
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Pilocarpine & Carbachol
- increase outflow of aqueous humor via ciliary muscle contraction & opening of trabecular meshwork |
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Trazodone
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inhibits serotonin reuptake
- atypical depression & insomnia - toxicity: sedation, nausea, priapism & postural hypotension |
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Maprotiline
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blocks NE reuptake
- atypical depression - toxicity: sedation & orthostatic hypotension |
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Mirtazapine
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alpha-2 antagonist & 5-HT2 and 5-HT3 receptor antagonist
- atypical depression - toxicity: sedation, increased appetite, weight gain & dry mouth |
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Bupropion
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increases NE and Dopamine
- atypical depression & smoking cessation - toxicity: tachycardia, insomnia, headache, seizure in bulimics - NO sexual side effects |
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list of MAO inhibitors
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Tranylcypromine
Phenelzine Isocarboxazid Selegiline |
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toxicity of MAO inhibitors
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Hypertensive crisis (ingestion of tyramine)
CNS stimulation |
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list of TCAs
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Amitriptyline
Imipramine Doxepin Amoxapine |
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drug used for bedwetting
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Imipramine
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drug used for OCD
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Clomipramine
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side effects of TCAs
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Convulsions, Coma, Cardiotoxicity
- sedation, postural hypotension, hyperpyrexia and respiratory depression - confusion & hallucinations in elderly |
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which TCA should be given to elderly?
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Nortriptyline
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TCA overdose cardiotoxicity
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NaHCO3
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Venlafaxine
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inhibits Serotonin & NE reuptake
- depression, generalized anxiety & panic disorders - toxicity: increased BP |
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Duloxetine
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inhibits Serotonin & NE reuptake
- depression, Diabetic Peripheral Neuropathy - toxicity: increased BP |
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list of SSRIs
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Fluoxetine
Paraxetine Setraline Citalopram |
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SSRI toxicity
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- GI distress
- sexual dysfunction - Serotonin Syndrome = hyperthermia, confusion, myoclonus, CV collapse, flushing, diarrhea & seizures |
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treatment for Serotonin Syndrome
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Cyproheptadine
- 5-HT2 receptor antagonist |
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Buspirone
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stimulates 5-HT1A receptors
- Generalized Anxiety - NO sedation, addiction or tolerance - takes 1-2 weeks to take effect - does not interact with alcohol |
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Lithium
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inhibitor of phosphoinositol
- toxicity: tremor, sedation, edema, heart block, hypothyroidism, polyuria (NDI) |
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drug that causes Ebstein anomaly
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Lithium
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Ziprasidone toxicity
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prolong QT interval
- atypical antipsychotic |
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Clozapine toxicity
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agranulocytosis & weight gain
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Risperidone toxicity
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hyperprolactinemia
- ammenorrhea |
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list of Atypical Antipsychotics
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Olanzapine
Clozapine Quetiapine Risperidone Aripiprazole Ziprasidone |
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Tardive Dyskinesia
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stereotypic oral-facial movements
- result from long-term antipsychotic use |
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Neuroleptic Malignant Syndrome
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fever, encephalopathy, vitals unstable, elevated enzymes, rigidity of muscles
- result of antipsychotic use |
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treatment for Neuroleptic Malignant Syndrome
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Dantrolene
- D2 agonist |
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Chlorpromazine toxicity
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corneal deposits
- antipsychotic |
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Thioridazine toxicity
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retinal deposits
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Extrapyramidal system side effects
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hours = acute dystonia (muscle spasm, stiffness)
days = akathisia (restlessness) weeks = bradykinesia months = tar dive dyskinesia |
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list of Antipsychotics
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Haloperidol + "-azines"
- block D2 receptors = increase cAMP |
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Antipsychotic toxicity
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- galactorrhea
- dry mouth, constipation - sedation, hypotension - EPS |
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ADHD
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Methylphenidate, Amphetamine
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PTSD
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SSRIs
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Tourette's Syndrome
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Haloperidol, Risperidone
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