Cns Pharmacology

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Properties of benzodiazepines

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Bind to gamma subunit of GABA(A) complex to increase frequecy of Cl- channel opening; no GABAmimetic activity; BZ1 mediates sedation; BZ2 mediates antianxiety and impairment of cognitive functions

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Benzodiazepine drugs

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Alprazolam, diazepam, lorazepam, midazolam, temazepam, oxazepam

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Uses of alprazolam

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Anxiety, phobias, panic attacks

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Uses of diazepam

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Anxiety, preop sedation, muscle relaxation, withdrawal states

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Uses of lorazepam

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Anxiety, preop sedation, status epilepticus

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Uses of midazolam

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Preop sedation and anesthesia, anterograde amnesia

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Uses of temazepam

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Sleep disorders

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Uses of oxazepam

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Sleep disorder and anxiety

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Pharmacokinetics of benzodiazepines

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Liver metabolized to active compounds except oxazepam, temazepam, lorazepam; t1/2: diazepam > lorazepam > alprazolam > temazepam > oxazepam > midazolam

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Uses of barbiturates

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Phenobarbital for seizures; thiopental for induction of anesthesia

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Properties of barbiturates

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Prolong GABA activity; increase duration of Cl- channel opening; GABAmimetic activity at high doses; bind to beta subunit of GABA(a) complex; inhibit complex I of ETC

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Pharmacokinetics of barbiturates

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General inducers of P450; contraindicated in porphyrias

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Withdrawal signs of benzodiazepines

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Rebound insomnia, anxiety, seizures

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Withdrawal signs of barbiturates and ethanol

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Anxiety, agitation, life threatening seizures

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Drug interactions of GABAa drugs

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Life threatening respiratory depression if used with other CNS depressants (antihistaminics, opiates, beta blockers); Barbiturates induce metabolism of lipid-soluble drugs (oral contraceptives, carbamazepine, phenytoin, warfarin)

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Flumazenil

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Benzodiazepine receptor antagonist. Used as antidote for benzodiazepine overdose.

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Zolpidem

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BZ1 receptor agonist used in sleep disorders. No cognitive impairment (no BZ2 actions), overdose reversed by flumazenil, less tolerance and abuse liability

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Buspirone

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No effect on GABA, 5-HT1a partial agonist, used for generalized anxiety, nonsedative, 1-2 weeks for effects

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Effects of alcohols

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GABA mimetic activity causes CNS depression; metabolic acidosis; fetal alcohol syndrome

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Metabolism of ethylene glycol

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Ethylene glycol + alcohol DH --> glycoaldehyde + aldehyde DH --> glycolic acid --> oxalic acid

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Effects of ethylene glycol

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CNS depression, severe metabolic acidosis, nephrotoxicity

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Metabolism of methanol

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Methanol + alcohol DH --> formaldehyde + aldehyde DH --> formic acid

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Effects of methanol

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Respiratory failure, severe anion gap metabolic acidosis, ocular damage

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Treatment of alcohol overdose

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Fomepizole (alcohol DH inhibitor) and hemodialisis

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Metabolism of ethanol

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Ethanol + alcohol DH --> acetaldehyde + NADH + acetaldehyde DH --> acetic acid + NADH

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Effects of ethanol

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CNS depression, metabolic acidosis, acetaldehyde toxicity

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Acetyldehyde toxicity

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Nausea, vomit, headache, hypotension, inactivates folate, decreases availability of thiamine

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Drugs that cause disulfram-like effects

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Disulfram-like effects = acetaldehyde toxicity. Disulfram inhibits acetaldehyde DH. Metronidazole, cefamandole, cefoperazone, cefotetan, chlorpropamide

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Anticonvulsant drugs

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Phenytoin, carbamazepine, benzodiazepines, barbiturates, lamotrigine, topiramate, felbamate, ethosuximide, valproic acid

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Drugs used for partial seizures

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Valproic acid, phenytoin, carbamazepine

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Drugs used for general tonic-clonic seizures

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Valproic acid, phenytoin, carbamazepine

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Drugs used for general absence seizures

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Ethosuximide

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Drugs used for status epilepticus

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Lorazepam, diazepam, phenytoin

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Phenytoin MOA

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Inhibits fast Na channels in axons which decreases conduction and prevents seizure propagation

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Pharmacokinetics of phenytoin

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Variable absorption, nonlinear kinetics at low doses, zero-order kinetics at high doses, inducer of P450

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Phenytoin side effects

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CNS depression, gingival hyperplasia, hirsutism, osteomalacia (decreases vitamin D), megaloblastic anemia (decreases folate), aplastic anemia, teratogenic (cleft lip and palate).

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Carbamazepine MOA

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Inhibits fast Na channels in axons which decreases conduction and prevents seizure propagation

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Pharmacokinetics of carbamazepine

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Induces P450

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Carbamazepine side effects

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CNS depression, osteomalacia, megaloblastic anemia, aplastic anemia, exfoliative dermatitis, increases ADH secretion (dilutional hyponatremia), teratogenic (cleft lip and palate, spina bifida)

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Valproic acid MOA

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Inhibits fast Na channels in axons which decreases conduction and prevents seizure propagation; Inhibits GABA transaminase; Blocks presynaptic Ca+ channels

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Uses of valproic acid

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Seizures, bipolar mania, migraines

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Pharmacokinetics of valproic acid

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Inhibits P450

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Valproic acid side effects

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Hepatotoxic metabolite, thrombocytopenia, pancreatitis, alopecia, spina bifida

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Ethosuxamide MOA

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Blocks presynaptic T-type Ca+ channels in thalamic neurons

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Lamotrigine MOA

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Blocks Na+ channels and glutamate receptors. Side effect: Steven-Johnson

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Inhaled anesthetic drugs

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Nitrous oxide, halothane

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Properties of halothane

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High potency (0.8% MAC), high blood-gas ratio (2.3), sensitizes heart to catecholamines

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Side effects of halothane

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Malignant hyperthermia, hepatitis, cardiac arrhythmias

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What is MAC?

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Minimal alveolar concentration is the amount of anesthetic at which 50% of patients don't respond to surgical stimulus. Analogous to ED50, measures potency, the more lipid soluble the lower the MAC, lower in elderly

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What is the blood-gas ratio?

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Measure of the onset of recovery. The more soluble in the blood the slower the anesthesia and recovery.

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Intravenous anesthetic drugs

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Midazolam, thiopental, propofol, fentanyl, ketamine

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General anesthesia protocol

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Includes sedation and anterograde amnesia (midazolam), induction (propofol), analgesia (fentanyl), muscle relaxant for intubation (succinylcholine) and may or may not include atropine in case of CV depression due to propofol

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Naloxone

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Antidote for opiods

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Neostigmine

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AChE inhibitor reverses non-depolarizing muscle relaxants

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What are the ester local anesthetics?

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Procaine, cocaine, benzocaine. Metabolized by plasma esterases. All have only one "i"

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What are the amide local anesthetics?

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Lidocaine, bupivacaine, mepivacaine. Metabolized by liver amidases. All have two "i".

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MOA of local anesthetics

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Nonionized form crosses axonal membrane --> ionized form blocks inactivated Na+ channel --> prevent propagation of action potentials

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Side effects of local anesthetics

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Neurotoxicity, cardiovascular toxicity, allergies. Use alpha-1 agonists to prevent absorption.

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Skeletal muscle relaxants MOA

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Nicotinic antagonists (competitive, nondepolarizing); Nicotinic agonists (noncompetitive, depolarizing)

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Non-depolarizing muscle relaxant drugs

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Atracurium, mivacurium, tubocurarine

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Non-depolarizing muscle relaxant properties

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Nicotinic antagonists, reversible with AChE inhibitors, progressive paralysis, no effects on heart or CNS

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Properties of succinylcholine

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Depolarizing muscle relaxant, nicotinic agonist; Phase I: depolarization, fasciculation, flaccid paralysis; Phase II: desensitization. Caution in atypical pseudocholinesterase, hyperkalemia, malignant hyperthermia

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Malignant hyperthermia

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Succinylcholine side effect in genetically susceptible people. Muscle rigidity, hyperthermia, hypertension, acidosis, hyperkalemia. Rx.: dantrolene

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Opiod analgesic drugs

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Morphine, meperidine, methadone, codeine, fetanyl, heroin

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Contraindications of opiod analgesics

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Head injuries, pulmonary dysfunction, hepatic or renal dysfunction, adrenal or thyroid deficiencies, pregnancy

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Effects of morphine

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Analgesia, sedation, respiratory depression (decreased response to PCO2), miosis, cough supression, nausea, vomiting

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Pharmacokinetics of morphine

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Phase 2 metabolism by glucoronidation. Caution in renal dysfunction as morphine-6-glucoronide is highly active

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Opiod toxicity

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Pinpoint pupils, repiratory depression and coma. Rx. Naloxone

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Meperidine

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Opiod without miosis or spasms. Metabolized via P450 to normeperidine which can cause seizures

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Methadone

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Used for opiate withdrawal in addicts

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Codeine

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Cough suppressant, analgesia, use in combination with NSAIDs

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Symptoms of opiod withdrawal

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Yawning, lacrimation, rhinorrea, salivation, anxiety, muscle spasms and CNS-originating pain. Rx.: methadone

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Drugs used in Parkinson disease

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Levodopa, tolcapone, selegiline, bromocriptine, benztropine, amantadine

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Levodopa

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Crosses CNS barrier. Converted to dopamine in CNS and periphery, so use tolcapone, carbidopa and selegiline

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Tolcapone

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Inhibits COMT which blocks levodopa conversion to methyldopa which has no pharm actions

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Carbidopa

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Inhibits conversion of levodopa to dopamine in peripheral tissues, increasing CNS availability

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Selegiline

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MAOb selective inhibitor, adjunt to levodopa to decrease dopamine metabolism in CNS

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Bromocriptine

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Dopamine receptor agonist used in hyperprolactinemia, acromegaly

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Benztropine

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Muscarinic blocker used to decrease Ach activity in Parkinson. Decreases tremor and rigidity but not bradykinesia

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Atypical antipsychotics

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Clozapine, olanzapine, risperidone, aripiprazole

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Atypical antipsychotic MOA

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Inhibition of dopamine and 5HT2 receptors

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Side effects of antipsychotic drugs

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Extrapyramidal symptoms, akathisia, tardive dyskinesia, dysphoria, endocrine dysfunction, weight gain, hypotension, muscarinic blockade tachychardia

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Specific side effects of thioridazine

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Torsades, retinal deposits

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Typical antipsychotics

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Chlorpromazine, thioridazine, fluphenazine, haloperidol

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Specific side effects of haloperidol

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Neuroleptic malignant syndrome, tardive diskynesia

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Specific side effects of clozapine

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Agranylocytosis, seizures, salivation

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MAO inhibitor drugs

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phenelzine, tranylcypromine

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Drug interaction of MAO inhibitors

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Tyramine, TCAs, alpha-1 agonists, levodopa: increase NE --> hypertensive crisis; Serotonin syndrome with SSRI, TCA, meperidine --> sweating, rigidity, myoclonus, hyperthermia

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Tricyclic antidepressant drugs

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Amitriptyline, imipramine, clomipramine

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TCAs MOA

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Nonspecific blockade of 5HT and NE reuptake

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Side effects of TCAs

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Muscarinic blockade, alpha blockade, serotonin syndrome, hypertensive crisis

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SSRI drugs

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Fluoxetine, sertraline, paroxetine

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Side effects of SSRI

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Anxiety, agitation, bruxism, sexual dysfunction, weight loss

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Serotonin syndrome

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Sweating, rigidity, myoclonus, hyperthermia. Interaction between MAOi, TCAs, SSRIs, meperidine, dextromethorphan

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Drug-induced hypertensive crisis

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Due to interaction between MAOi, TCAs, alpha-1 agonists

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Venlafaxine

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Selective reuptake inhibitor of NE and 5HT. Can cause hypertensive crisis and serotonin syndrome

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Bupropion

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Dopamine reuptake blocker. Used in smoking cessation

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Lithium MOA

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Prevents recycling of inositol (decreases PIP2), decreases cAMP

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Lithium side effects

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Narrow therapeutic index requires monitoring, tremor, hypothyroidism (decreases TSH effects and inhibits 5'-deiodinase), nephrogenic diabetes insipidus (manage with amiloride), teratogenic

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Methylphenidate

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Reuptake inhibitor and releaser of DA and NE. Side effects: agitation, restlessness, insomnia, CV toxicity. Treats ADHD.

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Atomoxetine

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Selective NE reuptake inhibitor. Treats ADHD.