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66 Cards in this Set
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Epinephrine
Brimonidine |
Glaucoma
α-agonist: ↓aqueous humor synthesis do NOT use epi in closed-angle glaucoma |
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Timolol
Betaxol Carteolol |
Glaucoma
β-blocker: ↓aqueous humor secretion contra: asthma, COPD |
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Acetazolamide
Dorzolamide |
Glaucoma diuretic
Carbonic anhydrase inhibitor: ↓aqueous humor secretion due to↓HCO3 |
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Pilocarpine
Carbachol |
Glaucoma
Direct cholinomimetic: contract ciliary muscle and open trabecular meshwork into canal of Schlemm Pilocarpine- for EMERGENCIES |
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Physostigmine
Echothiophate |
Glaucoma
Indirect cholinomimetic: contract ciliary muscle and open trabecular meshwork |
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Latanoprost
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Glaucoma
Prostaglandin (PGF2α): ↑outflow SE: darkening of iris |
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Morphine
Fentanyl Codeine Heroin |
Opiod agonists
Pain, acute pulmonary edema Tox: addiction, respiratory depression, constipation, miosis, CNS depression, tolerance Tolerance to constipation and miosis does not readily occur |
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Meperidine
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Opiod agonist- fast acting
Pain, acute pulmonary edema Tox: addiction, respiratory depression, CNS depression M receptor blocker: NO MIOSIS or smooth muscle contraction |
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Dextromethorphan
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Opiod agonist
Cough suppressent |
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Loperamide
Diphenoxylate |
Opiod agonists
Diarrhea |
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Methadone
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Opiod agonist
Maintenance programs for addicts due to long 1/2 life |
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Nalaxone
Naltrexone |
Opiod antagonist
Opiod agonist toxicity Greatest affinity to µ receptor |
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Ketamine
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NMDA receptor antagonist
Reverses opiod tolerance |
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Butophanol
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Partial µ opiod agonist, full κ agonist
Pain- less respiratory depression Tox: withdrawal if on full opiod agonist |
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Tramadol
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Very weak opiod agonist; inhibits 5HT and NE reuptake (tram it all)
Chronic pain Tox: similar to opiods, seizures |
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Phenytoin
Fosphenytoin |
Seizures: partial, tonic-clonic (1st), status epilepticus (prophylaxis)
Na channel blockade: ↑refractory period & ↓glutamate release Tox: cosmetic effects (thus less compliance) such as SLE-like syndrome, gingival hyperplasia, generalized lymphadenopathy; megaloblastic anemia, TERATOGENIC, P450 inducer, nystagmus, ataxia, sedation Fosphenytoin: parenteral use |
Also a Class IB Antiarrhythmic
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Carbamazepine
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Seizures: partial, tonic-clonic (1st); trigeminal neuralgia
Na channel blockade: ↑refractory period Tox: AGRANULOCYTOSIS, SIADH, teratogenic, P450 inducers, Stevens-Johnson Syndrome, diploplia, ataxia, liver tox. |
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Lamotrigine
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Seizures: partial, tonic-clonic
Na channel blockade: ↑refractory period Tox: Stevens-Johnson Syndrome |
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Gabapentin
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Seizures: partial, tonic-clonic
Inhibits voltage dependent Ca channels Tox: sedation, ataxia |
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Topiramate
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Seizures: partial, tonic-clonic
Na channel blockade, ↑GABA receptor action Tox: kidney stones, weight loss, sedation, mental dulling |
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Phenobarbital
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Seizures: partial, tonic-clonic
1st line in pregnancy and children Barbituate: ↑GABA receptor action Tox: P450 inducer, sedation, tolerance, dependence, precipitation of intermittent porphyria |
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Valproic acid
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Seizures: partial, tonic-clonic(1st), absence, myoclonic
Na channel blockade, ↑GABA concentration Tox: NEURAL TUBE DEFECTS (spina bifida), fatal HEPATOTOX, GI distress, tremor, weight gain Contra: pregnancy |
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Ethosuximide
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Seizures: absence (1st)
Blocks T-type thalamic Ca2+ channels Tox: Stevens-Johnson syndrome, GI distress, fatigue, headache, urticaria |
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Diazepam
Lorazepam |
Seizures: acute status epilepticus (1st)
Benzodiazepines: ↑GABA receptor action Tox: sedation, tolerance, dependence |
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Tiagabine, Vigabatrin, Levetiracetam
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Seizures: partial, tonic-clonic
↑GABA concentration newer anticonvulsant drugs |
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Partial Seizure- simple or complex
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1st line: valproic acid, phenytoin, carbamazepine
Pregnancy: phenobarbital |
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Tonic-Clonic Seizure
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1st line: valproic acid, phenytoin, carbamazepine
Pregnancy: phenobarbital |
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Myoclonic Seizure
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1st line: valproic acid
Alternate: benzodiazepines |
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Absence Seizure
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1st line: ethosuxamide
Alternate: valproic acid |
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Status Epilepticus
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Prophylaxis: phenytoin
Acute: diazepam or lorazepam |
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Phenobarbital
Pentobarbital Thiopental Secobarbital |
Barbituates: GABA-A receptor agonist= ↑Cl channel open= ↓ neuron firing
Anxiety, seizures, insomnia, induction of anesthesia (thiopental) Tox: dependence, CNS depression, respiratory depression, COMA, P450 inducer Overdose: symptomatic mgmt, assist respiration Contra: porphyria |
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Benzodiazepine Class
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GABA-A receptor agonist= ↑FREQUENCY of Cl channel opening= ↓ neuron firing
Anxiety, spasticity, status epilepticus, detoxication, night tremors, sleep walking, general anesthetic, muscle relaxant, hypnotic Tox: dependence, CNS depression, less risk of coma and respiratory depression than barbiturates |
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Flumazenil
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Benzo overdose
Competitive antagonist at GABA-A receptor's benzo site |
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Chlorodiazopoxide
Clorazepate Diazepam Flurazapam |
Long-acting Benzo
↑risk of falls, ↓risk of addiction |
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Midazolam
Oxazepam Alprazolam Triazolam |
Short-acting Benzo (MOAT)
↓risk of falls, ↑risk of addiction |
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General Principles of Anesthetics
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drugs with ↑solubility in lipids= ↑potency
Factors affecting inhaled anesthetics: Inspired air: ↓MAC= ↑potency Lungs: rate and depth of ventilation Blood: ↑solubility (blood/gas partition coefficient)= slower onset of action and slower recovery time Target tissues: ↑arteriovenous gradient= slower onset of action |
Inhaled Anesthetics Effects:
Cardiovascular: myocardial depression= ↓CO and hypotension Respiratory: depression (except NO) Brain: ↓vascular resistance= ↑cerebral blood flow ↓renal blood flow, ↓GFR, ↓hepatic blood flow |
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Halothane
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Inhaled anesthetic
slow induction/recovery, high potency For Asthmatics- has bronchodilation property Tox: hepatotox, malignant hyperthermia, cardiac arrythmias |
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Enflurane
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Inhaled anesthetic
Tox: tonic-clonic muscle spasms, malignant hyperthermia |
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Isoflurane
Sevoflurane |
Inhaled anesthetic
Sevoflurane has bronchodilation property Tox: malignant hyperthermia |
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Methoxyflurane
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Inhaled anesthetic
Tox: nephrotoxic, malignant hyperthermia |
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Nitrous oxide
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Inhaled anesthetic
fast induction/recovery, low potency Tox: expansion of trapped gas, NO malignant hyperthermia |
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Malignant Hyperthermia
Treatment? |
Hypersensitivity of skeletal muscles to inhalation anesthetics (especially halothane) + succinylcholine
Auto Dominant trait: defect of ryanodine receptors of the sarcoplasmic reticulum Symptoms after surgery: fever, muscle rigidity, tachycardia, hypertension, myoglobinemia Treatment: DANTROLENE- acts on ryanodine receptors to prevent release of Ca from sarcoplasmic reticulum |
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Thiopental
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IV Anesthetic: Barbiturate
Induction of anesthesia & short surgical procedures ↑potency, ↑lipid solubility, rapid entry into brain effect terminated by rapid distribution into tissue and fat ↓cerebral blood flow |
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Midazolam
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IV Anesthetic: Benzodiazepine
Endoscopy |
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Ketamine
PCP Analogs |
IV Anesthetic: block NMDA receptors
Disorientation, hallucination, bad dreams, ↑cerebral blood flow Only anesthetic that STIMULATES cardiovascular |
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Morphine
Fentanyl |
IV Anesthetic: Opiods
General anesthesia |
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Propofol
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IV Anesthetic: potentiates GABA-A receptor
Rapid anesthesia induction, short procedures Less post-op nausea than thiopental |
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Local Anesthethics
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Block Na+ channels: bind to receptor on inner portion of channel
Preferentially bind to activated Na channels: most effective in rapidly firing neurons Order of nerve blockade: small myelinated> small unmyelin> large myelin> large unmyelin Order of loss: pain(1st)> temp> touch> pressure |
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Procaine
Cocaine Tetracaine |
Esters
Local Anesthesia Except for cocaine, give w/epinephrine Tox: CNS excitation, hypertension, hypotension, arrhythmias (cocaine) |
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Lidocaine
Mepivacaine Bupivacaine |
AmIdes (have to I's in name)
Local Anesthesia Give w/epi Give amides if allergic to esters. Tox: CNS excitation, hypertension, hypotension, severe cardiovasc tox (bupivacaine) |
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Succinylcholine
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Motor nicotinic receptor blocker
Muscle paralysis in surgery, mechanical ventilation SE: hypercalcemia, hyperkalemia Blockade reversal: Phase I (prolonged depolarization)- no antidote; cholinesterase inhibitors will potentiate block Phase II (repolarized)- cholinesterase inhibitors |
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Tubocurarine
Atracurium Mivacurium Pancuronium Vecuronium Rocuronium |
Motor nicotinic receptor blocker
Competitive w/Ach Muscle paralysis in surgery, mechanical ventilation Blockade reversal: cholinesterase inhibitors |
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Parkinson's Disease Drugs
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BALSA:
Bromocriptine & other dopamine agonists Amantadine Levodopa + Carbidopa Selegiline & COMT inhibitors Antimuscarinic (Benztropine) |
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Bromocriptine
Pergolide |
Partial dopamine agonist: ergot alkaloid
Parkinson's disease |
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Pramipexole
Ropinirole |
Partial dopamine agonist: non-ergot alkaloid (preferred over ergot)
Parkinson's disease |
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Amantadine
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↑dopamine release
Parkinson's disease Tox: ataxia |
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Levodopa
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Unlike dopamine, L-dopa crosses blood-brain barrier and is converted by dopa decarboxylase to dopamine
Parkinson's disease Vitamin B6 increases peripheral metabolism Tox: arrhythmia from peripheral conversion, dyskinesia after dose, akinesia between doses, On-off effect (drug efficacy is unpredictable) |
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Selegiline
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Selectively inhibits MAO-B (which preferentially metabolizes dopamine)
Parkinson's disease Tox: enhanced L-dopa effects |
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Entacapone
Tolcapone |
COMT inhibitor: prevent L-dopa degradation
Parkinson's disease |
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Memantine
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NMDA receptor antagonist
Alzheimer's disease (MEMory) Tox: dizziness, confusion, hallucinations |
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Donepezil
Galantamine Rivastigmine |
Acetylcholinesterase inhibitors
Alzheimer's disease Tox: nausea, dizziness, insomnia |
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Huntington's drugs
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Resperine + tetrabenazine: amine depleting
Haloperidol: dopamine antagonist |
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Sumatriptan
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5HT-1B and 5HT-1D agonists: vasoconstriction, inhibition of trigeminal activation, inhibition of vasoactive peptide release
Acute migraine, cluster headaches Tox: coronary vasospasm |
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Essential Tremor
Treatment? |
Familial tremor that is apparent during voluntary movements
Rx: β-blocker (propranolol) |
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Carbidopa
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PERIPHERAL decarboxylase inhibitor; ↑bioavailability of L-dopa in brain and ↓ peripheral side effects
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Lamotrigine
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Newer seizure med: GABA mechanism
Partial refractory seizures SE: skin rash |
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