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Opioids
- Morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
- Agonists at opioid receptors - open K channels, close Ca channels -> decrease synaptic transmission
- Pain, cough suppression, diarrhea, pulmonary edema, maintenance for addicts
- Respiratory depression, constipation, miosis (pinpoint pupils), CNS depression
- Treat toxicity with naloxone or naltrexone
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Butorphanol
- Partial agonist at opioid mu receptors, agonist at kappa receptors
- For pain
- Less respiratory depression than full agonists
- Causes withdrawal if on full opioid agonist
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Tramadol
- Weak opioid agonist; inhibits 5-HT3 and NE uptake
- Chronic pain
- Toxicity similar to opioids; decreases seizure threshold
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First line for tonic-clonic seizures
- Phenytoin
- Valproic acid
- Carbamazepine
- (Peeing and Very Convulsive)
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First line for absence seizures
Ethosuximide
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First line for prophylaxis of status epilepticus
Phenytoin
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First line for acute status epilepticus
Benzodiazepines (diazepam or lorazepam)
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First line for trigeminal neuralgia
Carbamazepine
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First line for seizures in pregnant women, children
Phenobarbital
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Phenytoin
- Block Na channels, increase refractory period, inhibit glutamate release
- Tonic-clonic seizures (also class IB antiarrythmic)
- SLE-like syndrome, induction of P450
- Chronic use: gingival hyperplasia, peripheral neuropahy, hirsutism, megaloblastic anemia
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Thiopental
- Barbituate
- Increase duration of Cl channel opening -> increase GABA -> decrease neuron firing
- Induction of anesthesia
- Recovery from anesthesia is from redistribution in tissues
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Phenobarbital, pentobarbital, secobarbital
- Barbituates
- Increase duration of Cl channel opening, increase GABA action, decrease neuron firing
- Anxiety, seizures, insomnia
- Dependence, CNS depression w/alcohol, respiratory/CV depression, induction of P450
- Contraindicated in porphyria
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Benzodiazepines
- -zepams and alprazolam
- Increase frequency of Cl channel opening
- Anxiety, spasticity, status epilepticus (lorazepam and diazepam), alcohol withdrawal, general anesthetic
- Dependence, CNS depression w/alcohol, less respiratory depression than barbs
- Treat overdose with flumazenil
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Halothane
- Inhaled anesthetic
- Also -fluranes and nitrous oxide
- Myocardial depression, respiratory depression, decreased cerebral blood flow
- Hepatotoxicity (halothane), malignant hyperthermia
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Midazolam
- Benzodiazepine used for endoscopy
- Treat overdose with flumazenil
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Ketamine
- IV anesthetic, blocks NMDA receptors
- Cause disorientation, hallucination, bad dreams
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Opiates for IV anesthesia
Morphine, fentanyl
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Propofol
Rapid anesthesia induction and short procedures
-
Local anesthetics
- Esters: one I (procaine); amides: two Is (lidocaine)
- Block Na channels in rapidly firing neurones
- Order of sensory loss: pain, temp, touch, pressure
- Used for minor surgical procedures and spinal anesthesia
-
Succinylcholine
- Depolarizing neuromuscular blocker
- Rapid sequence intubation
- Can cause hypercalcemia and hyperkalemia
- Can be reversed after repolarization by neostigmine
-
Tubocurarine
- Nondepolarizing neuromuscular blocker
- Compete with ACh for receptors
- Reversed with cholinesterase inhibitors (neostigmine)
-
Dantrolene
- Treat malignant hyperthermia (cause by inhaled anesthetics + succinylcholine)
- Also treats neuroleptic malignant syndrome (toxicity of antipsychotics)
- Prevents release of Ca from SR
-
L-dopa/carbidopa
- Used in Parkinson's
- Increases level of dopamine in brain; crosses BBB and is converted by dopa decarboxylase in CNS to dopamine
- Carbidopa limits peripheral side effects (arrythmia)
- Dyskinesia after administration and akinisia between doses
-
Selegiline
- Parkinson's dz
- Selectively inhibits MAO-B increasing availability of dopamine (prevents dopamine breakdown)
-
Bromocriptine
Dopamine agonist used in Parkinson's
-
Amantadine
- Used in Parkinson's
- Increases dopamine release
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Sumatriptan
- 5-HT IB/ID agonist
- Used for acute migraine and cluster headache attacks
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Methylphenidate
- = Ritalin
- Used in ADHD, mechanism unknown
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High potency antipsychotics/neuroleptics
- Haloperidol, trifluoperazine, fluphenazine
- Block dopamine D2 receptors
- Positive symptoms of schizophrenia, psychosis, acute mania, Tourette's
- Extrapyramidal side effects (dystonia, akinesia, akathisia, tardive dyskinesia)
- Neuroleptic malignant syndrome: fever, encephalopathy, vitals unstable, elevated enzymes, rigidity of muscles
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Low potency antipsychotics
- Thioridazine, chlorpromazine
- Block D2 receptors
- Positive symptoms of schizophrenia, psychosis, acute manie, Tourette's
- Endocrine side effects - galactorrhea
- No extrapyramidal side effects
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Atypical antipsychotics
- It's atypical for old closets to quietly risper
- Olanzapine, clozapine, quietapine, risperidone
- Block 5-HT2, alpha, Ha and dopamine receptors
- Positive and negative symptoms of schizophrenia
- Olanzapine for OCD, anxiety disorder, depression, mania, Tourette's syndrome
- Clozapine may cause agranulocytosis
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Lithium
- Mood stabilizer for bipolar disorder - blocks relapse and acute manic events; treats SIADH
- Nephrogenic DI, hypothyroidism, Ebstein's anomaly in pregnancy (apically displaced tricuspid valve, ASD, atrialization of RV)
-
Buspirone
- Stimulates %-HT1A receptors
- Used for generalized anxiety disorder
- Non-addictive, non-sedating alternative to barbs and benzos
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Amitriptyline, Imiprimine
- Block reuptake of NE and serotonin
- Major depression, OCD, fibromyalgia
- Anticholinergic effects (tachycardia, urinary retention), Tri-Cs (Convulsions, Coma, Cardiotoxicity)
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SSRIs
- Fluoxetine
- Depression, OCD, bulimia, social phobias
- Serotonin syndrome when combined with MAOIs: hyperthermia, muscle rigidity, CV collapse, flushing, diarrhea, seizures; treat with cyproheptadine
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MAOIs
- Phenelzine, selegiline
- Increase levels of amine neurotransmitters
- Atypical depression, anxiety, hypochondriasis
- Hypertensive crisis with tyramine ingestion (wine, cheese), serotonin syndrome when combined with SSRIs
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Buproprion
- Smoking cessation
- Can cause seizure in bulimic patients or those with existing seizure disorder
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