Drugs to know Flashcards
- CNS stimulant
- agonist at nicotinic neuronal receptor
- some people have a gene that impairs metabolism, protecting them addiction
- use common in schizo
Nicotine
- benzo
- *** for status epilepticus via slow IVP
- *** for seizures in CNS stimulant OD
- *** for anti-anxiety
- adjunctive in atonic and absence szs
- tolerance develops
- long half life
- rapid oral but poor IM
Diazepam (Valium)
- blocks voltage dependent sodium channels (VSSC)
- reduces repetitive sz firing
- good for tonic-clonic and partial sz’s
- food enhances absorption and reduces GI upset
- *** Strong inducer of P450
- nystagmus
- additive to other CNS depressants
- rash
- *** gingival hyperplasia
- OD = death
- inhibited by valproic acid
- vitamin K deficiency in newborn
Phenytoin (Dilantin)
Methylphenidate (Ritalin)
- CNS stimulant for ADHD
Divalproex (Depakote)
- anti-mania
- rapid loading
- a lot like valproic acid
Amitriptyline (Elavil)
- TCAD
- anti-M (blurred vision, constipation, dry mouth, urinary hesitancy, fuzzy thinking, aggravates glaucoma, paralytic ileus, delirium)
- anti-adrenergic SEs
- weight gain
- sexual dysfunction
- Orthostatic hypotension (α1 blockade)
- OD = BAD! sudden cardiac death, sz’s
- ***highly sedating
Diazepam (Valium)
- benzo
- *** for status epilepticus via slow IVP
- *** for seizures in CNS stimulant OD
- *** for anti-anxiety
- adjunctive in atonic and absence szs
- tolerance develops
- long half life
- rapid oral but poor IM
- antagonist at the benzodiazepine binding site –> reverse CNS effects of benzos (OD or for to hasten surgery recovery)
Flumazenil (Romazicon)
- Mixed postsynaptic antagonist-serotonin reuptake inhibitor
- ***very strong sedative – good for sleep aid in depressed pts
- dizziness, nausea, agitation
- orthostasis (via alpha-adrenergic blockade), ESP IN ELDERLY
- priapism
- OD = minor problems
Trazodone (Desyrel)
- atypical antipsychotic
- tx of negative symptoms
- ***agranulocytosis
- ***hypersalivation
- *** lowers sz threshold
- weight gain
- try other drugs first!
Clozapine (Clozaril)
Ramelteon (Rozerem)
- Agonist at melatonin MT1 and MT2 (superchiasmatic nucleus of the thalamus)
- induces sleep and regulates circadian rhythms
Nitrous oxide
- inorganic gas (volatile) inhaled general anesthetic
- low potency (MAC = 105%)
- adjunctive agent
- analgesic and anxiolytic
- rapid onset and recovery
Heroin
- Opioid agonist
- Naltrexone (Revia) and Buprenorphine (Subutex) block reinforcing effects but don’t change cravings
- death by respiratory depression
Carbamazepine (Tegretol)
- blocks voltage dependent sodium channels (VSSC)
- suppresses repetitive AP
- *** Strong inducer of P450
- dosed 2-3x daily
- *** tx for partial sz and mania
- inhibited by valproic acid
- vitamin K deficiency in newborn
- diplopia, ataxia, nausea/vomiting, drowsiness,
- ***hyponatremia
- *** Stevens-Johnson syndrome
Phenobarbital (Luminal)
- BARB
- enhances GABA inhibition
- ***inhibits glutamate via antagonism (VSCC)
- ***valproic acid inhibits this drug!
- *** causes resp. depression when used with diazepam
- *** inducer of CYP450
- irritability
- sedation
- ***interferes with learning
- a tx for partial seizures, generalized tonic-clonic seizures, and neonatal status epilepticus
- *** causes fetal malformations
- *** vitamin K deficiency in newborns
Clozapine (Clozaril)
- atypical antipsychotic
- tx of negative symptoms
- ***agranulocytosis
- ***hypersalivation
- weight gain
- try other drugs first!
- atypical antipsychotic
- ***best tx for bipolar depression
- sedation
- weight gain
Quetiapine (Seroquel)
- BARB
- enhances GABA inhibition
- ***inhibits glutamate via antagonism (VSCC)
- ***valproic acid inhibits this drug!
- *** causes resp. depression when used with diazepam
- *** inducer of CYP450
- irritability
- sedation
- ***interferes with learning
- tx for partial seizures, generalized tonic-clonic seizures, and neonatal status epilepticus
- *** fetal malformations
- *** vitamin K deficiency in newborns
Phenobarbital (Luminal)
- binds to and inhibits function of synaptic vesicle protein SV2A in Ca++-mediated neurotransmitter release; VSCC
- ***tx for grand mal and partial sz
- No P450 drug metabolism, minimal drug interactions
Levetiracetam (Keppra)
- TCAD
- anti-M (blurred vision, constipation, dry mouth, urinary hesitancy, fuzzy thinking, aggravates glaucoma, paralytic ileus, delirium)
- anti-adrenergic SEs
- weight gain, sexual dysfunction
- Orthostatic hypotension (α1 blockade)
- OD = BAD! via sudden cardiac death, sz’s
- ***highly sedating
Amitriptyline (Elavil)
- blocks T-type Ca++ channels
- *** first line for absence sz c
- omplete metabolism by CYP3A4
- gastric distress
- HA
- dizziness
- gum hypertrophy
Ethosuximide (Zarontin)
- benzo
- long half life
- minimal tolerance
- *** can accumulate in elderly/ hepatic problems
- *** daytime sedation
Flurazepam (Dalmane)
Escitralopram (Lexapro)
- SSRI
- no sedation
- agonist at CB1 receptor
- can increase heart rate, precipitate seizures in epileptics, increase potential for ketoacidosis in diabetics
- cognitive impairments
- withdrawal minimal
- psychosis (induces and makes existing worse)
- tx for pain, appetite loss, nausea/vomiting, MS, glaucoma
Marijuana
Methamphetamine
- CNS stimulant
- acts upon locus ceruleus
- increases NE release
- reverses DA transporter to release DA
- makes schizo worse
- SSRI
- no sedation
Escitralopram (Lexapro)
- NMDA antagonist
- dissociative anesthetic- IV
- allows responsivity and reflexes with catatonia, amnesia, and analgesia, esp. in kids
- worsens schizo
ketamine
- binds to GABA receptor to PROLONG its action AND directly initiates chloride current to depress glu
- ***induction phase of general anesthesia
- decrease delta sleep
- decrease duration of REM
- high risk of tolerance (fast- 1 week)
- low safety margin in therapeutic range: antianxiety, anticonvulsant, muscle relaxant, sedative, and hypnotic
- *** induce CYP450
- lethal OD
Barbiturates
Zolpidem (Ambien)
- Z drug (binds to alpha-1 subunit of GABA-Cl channel ONLY)
- half life = 2 hours –> short duration of action
- ***reduces sleep latency and nocturnal awakenings
- first line for insomnia
- minimal tolerance
- ***no rebound insomnia
- benzo
- short half-life
- less daytime sedation but + rebound insomnia
- rapid oral
- anterograde amnesia
- confusion
- bizzare behavior
- agitation
- hallucinations
Triazolam (Halcion)
Clonidine (Catapres)
- α2 adrenergic agonist
- alleviates symptoms of SNS overactivity (nausea / vomiting, cramps, sweating, tachycardia, and increased blood pressure) that occur during acute OPIOID withdrawal (3-4 doses/day)
Alcohol
- CNS depressant
- cross-dependence with benzos and barbs
- enhances GABA activity
- *** decreases glu at high doses
- most commonly abused and misused drug in the US
- metabolized in liver at constant rate
- moderately rapid tolerance
- Agonist at melatonin MT1 and MT2 (superchiasmatic nucleus of the thalamus)
- induces sleep and regulates circadian rhythms
Ramelteon (Rozerem)
- typical antipsychotic
- low potency
- less EPS but high ANS SEs:
- anti-M (dry mouth, sedation)
- α1-blockade (hypotension)
- antihistamine (sedation)
Chlorpromazine (Thorazine)
- CNS stimulant
- acts upon locus ceruleus
- increases NE release
- reverses DA transporter to release DA
- makes schizo worse
Methamphetamine
Flumazenil (Romazicon)
- antagonist at the benzodiazepine binding site –> reverse CNS effects of benzos (OD or for to hasten surgery recovery)
- SSRI
- *** inhibits P450 (CYP2D6)
- longer half life
- mild sedation
Fluoxetine (Prozac)
Bupropion (Wellbutrin, Zyban)
- NDRI and smoking cessasion tx
- dizziness, dry mouth, tremor, insomnia
- ***anxiety
- ***aggravates psychosis
- ***potential for sz’s
- *** NO sexual SEs or weight gain
Fluoxetine (Prozac)
- SSRI
- *** inhibits P450 (CYP2D6)
- longer half life
- mild sedation
- partial agonist at mu opioid receptor
- blocks reinforcing effects of heroin
- no ups and downs
- lose cravings
Buprenorphine (Subutex)
Cocaine
- CNS stimulant
- blocks DA reuptake (and possibly 5HT, NE)
- makes schizo worse
Buprenorphine (Subutex)
- partial agonist at mu opioid receptor
- blocks reinforcing effects of heroin
- no ups and downs
- lose cravings