Benzodiazepines- Potentiate GABAA receptors - ↑ the frequency of Cl- channel opening - Have no GABA mimetic activity - sedation, antianxiety, impairment of cognitive functions Toxicity: Sedation, anterograde amnesia ...
Barbiturateseg phenobarbital, thiopental - Prolongation of GABA activity - ↑ duration of Cl- channel opening - Have GABA mimetic activity at high doses - stimulate heme synthesis (contraindicated in porphyrias!) ...
Buspirone- non-benzodiazepine drug - no effect on GABA - 5HT1A partial agonist - used for generalized anxiety disorders - nonsedative - takes 1 to 2 weeks for effects
TCAsamitriptyline, imipramine, clomipramine - nonspecific blockade of 5HT and NE reuptake Uses:- major depressions- phobic and panic anxiety states- OCDs- neuropathic pain- enuresis Toxicity: the "3 Cs": ...
MAO inhibitorsphenelzine, moboclemide - irreversible inhibition of MAOA and MAOB - Use: atypical depressions Drug interactions:- Serotonin syndrome- ↑ NE: hypertensive crisis (↑ BP, arrhythmias, excitation, hyperthermia) ...
Lithium- DOC for bipolar disorders - usually antidepressants/antipsychotics also required - prevents recycling of inositol (↓PIP2), ↓cAMP - narrow therapeutic index (requires therapeutic monitoring)- tremor, ...
Levodopa- prodrug converted to dopamine by aromatic amino acid decorboxylase (AAAD) - given with carbidopa Side effects:- dysinesias- psychosis- hypotension- vomiting
SelegilineMAOB-selective inhibitor (no tyramine interactions) - initial treatment and adjunct to levadopa Side effects:- dyskinesias- psychosis- insomnia (metabolized to amphetamine)
BromocriptineDeopamine-receptor agonist Use: hyperprolactemia and acromegaly
Phenytoin- Blocks axonal Na+ channes in their inactivated state- Prevents seizure propagation Uses: seizure states Side effects:- CNS depression- Hirsutism- Osteomalacia (vitamin D ↓)- Megaloblastic anemia ...
Carbamazepine- Blocks axonal Na+ channels in their inactivated state (like phenytoin) Uses: seizure states Side effects:- CNS depression- Osteomalacia- Megaloblasstic anemia- teratogenic
GabapentinAnticonvulsant Used in seizure states, neuropathic pain
FelbamateAnticonvulsant - Blocks Na+ channels and glutamate receptors Uses: seizure states (often adjunct therapy) Side effects: aplastic anemia
EthosuximideBlockade of T-type Ca2+ channels in thalamic neurons Use: absence seizures
LamotrigineBlocks Na+ channels and glutamate receptors - used in various seizures Side effects: Stevens-Johnson syndrome
TopiramateBlocks Na+ cahnnels and glutamate receptors and enhances GABA activity - Used in focal seizures in adults and children > age 2 Side effects: weight loss
General features of anticonvulsant drug use- anticonvulsants are additive with other CNS depressants - avoid abrupt withdrawal (may precipitate seizures) - ↓ efficacy of oral contraceptives via induction of cytochrome 450
PropofolIntravenous anaesthetic - used for induction and maintenance of anaesthesia- CNS and caridiac depressant
Fentanyl- Opiate used for induction and maintenance of anaesthesia - depresses respiratory function
AtracuriumNondepolarizing skeletal muscle relaxant - nicotinic antagonist (no effects on cardiac and smooth muscle) - safe in hepatic or renal impairment - spontaneous inactivation to laudanosine
Succinylcholine- depolarizing skeletal muscle relaxant - nicotinic agonist - rapidly hydrolyzed by pseudocholinesterase: short duration Cautions:- malignant hyperthermia- hyperkalemia
Cocaine- blocks DA, NE and 5HT reuptake in CNS; local anesthetic action from Na+ channel blockade - increase NE: sympathomimetic effect- increase DA: psychotic episodes, paranoia, hallucinaions, dyskinesias, ...
Amphetamines- Blockade of reuptake of NE and DA, release amines from mobile pool, weak MAO inhibitors
Marijuana- interaction with CB1 and CB2 cannabinoid receptors in CNS and periphery - sedation, euphoria, ↑ HR, delusions, hallucinations, conjunctival irritation
FluoxetineSSRI - selective blockade of 5HT reputake Uses:- major depression- OCD- bulimia- anxiety disorders Toxicity: serotonin syndrome
SertralineSSRI - selective blockade of 5HT reputake Uses:- major depression- OCD- bulimia- anxiety disorders Toxicity: serotonin syndrome
CitalopramSSRI - selective blockade of 5HT reuptake Uses:- major depression- OCD- bulimia- anxiety disorders Toxicity: serotonin syndrome
FluvoxamineSSRI - selective blockade of 5HT reuptake Uses:- major depression- OCD- bulimia- anxiety disorders Toxicity: serotonin syndrome
ParoxetineSSRI - selective blockade of 5HT reuptake Uses:- major depression- OCD- bulimia- anxiety disorders Toxicity: serotonin syndrome
AmitriptylineTCA - nonspecific blockade of 5HT and NE reuptake Uses:- major depressions- phobic and panic anxiety states- OCDs- neuropathic pain Side effects: muscarinic and α blockade Toxicity: the 3 Cs: coma, convulsions, ...
ImipramineTCA - nonspecific blockade of 5HT and NE reuptake Uses:- major depressions- phobic and panic anxiety states- OCDs- neuropathic pain Side effects: muscarinic and α blockade Toxicity: the 3 Cs: coma, convulsions, ...
ClomipramineTCA - nonspecific blockade of 5HT and NE reuptake Uses:- major depressions- phobic and panic anxiety states- OCDs- neuropathic pain Side effects: muscarinic and α blockade Toxicity: the 3 Cs: coma, convulsions, ...