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
Marijuana
- 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
Barbiturates
- 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
- *** induces CYP450
- lethal OD
Zaleplon (Sonata)
- Z drug (binds to alpha-1 subunit of GABA-Cl channel ONLY)
- half life = 1 hour –> short duration of action
- dizziness, HA, somnolence
- **no rebound insomnia
- ** decreases time to sleep onset –> sleep aid for middle of the night awakenings
Halothane (Fluothane)
- Fluorinated hydrocarbon
- general anesthetic- inhaled
- ***high solubility in blood - moderately/high potency (MAC = 0.75%)
- not good analgesic
- respiratory and CV failure
- ***can cause liver damage
- ***can trigger malignant hyperthermia
Amphetamines
- CNS stimulant
- acts upon locus ceruleus
- increases NE release
- reverses DA transporter to release DA
- makes schizo worse
Triazolam (Halcion)
- benzo
- short half-life
- less daytime sedation but + rebound insomnia
- rapid oral
- anterograde amnesia
- confusion bizzare
- behavior
- agitation
- hallucination
- blocks VSSC and T-type Ca++ channels –> potentiation of GABA function
- tx for tonic-clonic sz, partial, absence, atypical sz
- inhibits metabolism of phenytoin, lamotrigine, phenobarbital, carbamazepine, ethosuximide
- ***fetal malformations
Valproate
- anti-manic, bipolar depression tx
- bad taste
- tremor
- *** narrow therapeutic window
- *** diabetes insipidus
- *** hypothyroidism
- 10-21 day onset
- *** diuretics and NSAIDs increase its plasma levels
- *** increased Na+ decreases its plasma levels
Lithium carbonate
- MAOI
- *** tyramine reaction –> HTN crisis
- *** postural hypotension
- OD = BAD! sz, shock, hyperthermia
- *** good for atypical depression
- dry mouth, constipation, urinary retention, sexual dysfunction, weight gain
Phenelzine (Nardil)
Benzodiazepines
- binds to GABA receptor to INTENSIFY its action via opening of chloride channels –> raise AP threshold
- NO induction of general anesthesia
- sleep and anxiolytic, panic disorder, generalized anxiety, social phobia, anticonvulsant
- daytime sedation, rebound insomnia
- performance impairment
- anterograde amnesia
- dependence/tolerance (slow)
- antagonist = Flumazenil (Romazicon)
Midazolam (Versed)
- benzo
- not much to note
Methadone
- long acting opioid agonist
- substitute for heroin to alleviate symptoms (no ups and downs, lose cravings)
- 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
Carbamazepine (Tegretol)
- benzo
- slow oral absorp.
- intermediate half life
- less depression of REM sleep
Temazepam (Restoril)
Levetiracetam (Keppra)
- 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
Haloperidol (Haldol)
- typical antipsychotic
- high potency
- tx of positive symptoms
- ***high EPS SEs (dystonia, akathisia, pseudoparkinsons, tardive dyskinesias)
CNS stimulant for ADHD
Methylphenidate (Ritalin)
- Z drug (binds to alpha-1 subunit of GABA-Cl channel ONLY)
- half life = 1 hour –> short duration of action
- dizziness, HA, somnolence
- ***no rebound insomnia
- *** decreases time to sleep onset –> sleep aid for middle of the night awakenings
Zaleplon (Sonata)
Temazepam (Restoril)
- benzo
- slow oral absorp.
- intermediate half life
- less depression of REM sleep
- benzo
- direct metabolism (no P450)
- short half life
- *** good for elderly and hepatic dysfunction
- slow oral absorp., good IM
- good for EtOH withdrawal, anti-anxiety, status epilepticus
Lorazepam (Ativan)
- opioid receptor antagonist
- blocks reinforcing actions of heroin but has no effect on craving
- reduces alcohol craving, consumption, and relapse rates when used in combination with psychotherapy
- can precipitate opioid withdrawal
Naltrexone (Revia)
- anti-mania
- rapid loading
- a lot like valproic acid
Divalproex (Depakote)
ketamine
- NMDA antagonist
- dissociative anesthetic- IV route
- allows responsivity and reflexes with catatonia, amnesia, and analgesia, esp. in kids
- worsens schizo
Nicotine
- CNS stimulant
- agonist at nicotinic neuronal receptor
- some people have a gene that impairs metabolism, protecting them from addiction
- use common in schizo
- 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)
Clonidine (Catapres)
Oxazepam (Serax)
- benzo
- direct metabolism (no P450)
- short half life
- *** good for elderly and hepatic dysfunction
- slow oral absorp.
- 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
Zolpidem (Ambien)
- antagonist at Histamine H1 and muscarinic cholinergic receptors
- sedation
- antimuscarinic in elderly
- *** treatment for acute dystonia (an EPS)
Diphenhydramine (Benadryl)
Disulfiram (Antabuse)
- inhibits aldehyde dehydrogenase (AIDH)
- causes 5-10x fold increase in acetaldehyde levels –> nausea/vomiting, respiratory and cardiovascular collapse, convulsions
- benzo
- direct metabolism (no P450)
- short half life
- *** good for elderly and hepatic dysfunction
- slow oral absorp.
Oxazepam (Serax)
- SNRI
- ***HTN
- ***anxiety
- *** more rapid withdrawal symptoms
- nausea, somnolence, sweating, dizziness, sexual dysfunction
Venlafaxine (Effexor)
Eszopiclone (Lunesta)
- Z drug (binds to alpha-1 subunit of GABA-Cl channel ONLY)
- half life = 6 hours (long)
- insomnia tx
- ***next-day psychomotor impairment
- *** NO tolerance
Trazodone (Desyrel)
- 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
- benzo
- rapid oral absorp.
- short half-life and effects
- good for elderly
- tx for panic disorder, acute anxiety
Alprazolam (Xanax)
Quetiapine (Seroquel)
- atypical antipsychotic
- ***best tx for bipolar depression
- sedation
- weight gain
- 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
Alcohol
- NDRI and smoking cessasion tx
- dizziness, dry mouth, tremor, insomnia
- ***anxiety
- ***aggravates psychosis
- ***potential for sz’s
- *** NO sexual SEs or weight gain
Bupropion (Wellbutrin, Zyban)
Ethosuximide (Zarontin)
- blocks T-type Ca++ channels
- *** first line for absence sz
- complete metabolism by CYP3A4
- gastric distress, HA, dizziness, gum hypertrophy
Paroxetine (Paxil)
- SSRI
- short half life
- *** withdrawal symptoms = flu-like/neurologic
- *** inhibits P450 (CYP2D6)
- mild sedation
Valproate
- blocks VSSC and T-type Ca++ channels –> potentiation of GABA function
- tx for tonic-clonic sz, partial, absence, atypical
- inhibits metabolism of phenytoin, lamotrigine, phenobarbital, carbamazepine, ethosuximide
- ***fetal malformations
- inhibits aldehyde dehydrogenase (AIDH)
- causes 5-10x fold increase in acetaldehyde levels –> nausea/vomiting, respiratory and cardiovascular collapse, convulsions
Disulfiram (Antabuse)
- CNS stimulant
- blocks DA reuptake (and possibly 5HT, NE)
- makes schizo worse
Cocaine
- Z drug (binds to alpha-1 subunit of GABA-Cl channel ONLY)
- half life = 6 hours (long)
- insomnia tx
- ***next-day psychomotor impairment
- *** NO tolerance
Eszopiclone (Lunesta)
Diphenhydramine (Benadryl)
- antagonist at Histamine H1 and muscarinic cholinergic receptors
- sedation
- antimuscarinic in elderly
- *** treatment for acute dystonia (EPS)
- long acting opioid agonist
- substitute for heroin to alleviate symptoms (no ups and downs, lose cravings)
Methadone
- binds to GABA receptor to INTENSIFY its action via opening of chloride channels –> raise AP threshold
- NO induction of general anesthesia
- sleep and anxiolytic, panic disorder, generalized anxiety, social phobia, anticonvulsant
- daytime sedation, rebound insomnia
- performance impairment
- anterograde amnesia
- dependence/tolerance (slow)
- antagonist = Flumazenil (Romazicon)
Benzodiazepines
Naltrexone (Revia)
- opioid receptor antagonist
- blocks reinforcing actions of heroin but has no effect on craving
- reduces alcohol craving, consumption, and relapse rates when used in combination with psychotherapy
- can precipitate opioid withdrawal
- Fluorinated hydrocarbon
- general anesthetic- inhaled
- ***high solubility in blood - moderately/high potency (MAC = 0.75%)
- not good analgesic
- respiratory and CV failure
- ***can cause liver damage
- ***can trigger malignant hyperthermia
Halothane (Fluothane)
- inorganic gas (volatile)
- inhaled general anesthetic
- low potency (MAC = 105%)
- adjunctive agent
- analgesic and anxiolytic
- rapid onset and recovery
Nitrous oxide
Phenelzine (Nardil)
- MAOI
- *** tyramine reaction –> HTN crisis
- *** postural hypotension OD = BAD! sz, shock, hyperthermia
- *** good for atypical depression
- dry mouth, constipation, urinary retention, sexual dysfunction, weight gain
- CNS stimulant
- acts upon locus ceruleus
- increases NE release
- reverses DA transporter to release DA
- makes schizo worse
Amphetamines
- typical antipsychotic
- high potency
- tx of positive symptoms
- ***high EPS SEs (dystonia, akathisia, pseudoparkinsons, tardive dyskinesias)
Haloperidol (Haldol)
- Opioid agonist
- Naltrexone (Revia) and Buprenorphine (Subutex) block reinforcing effects but don’t change cravings
- death by respiratory depression
Heroin
CNS stimulant for ADHD
d-Amphetamine (Adderall)
Chlorpromazine (Thorazine)
- typical antipsychotic
- low potency
- less EPS but high ANS SEs:
- anti-M (dry mouth, sedation)
- α1-blockade (hypotension)
- antihistamine (sedation)
Lorazepam (Ativan)
- benzo
- direct metabolism (no P450)
- short half life
- *** good for elderly and hepatic dysfunction
- slow oral absorp., good IM
- good for EtOH withdrawal, anti-anxiety, status epilepticus
Lithium carbonate
- anti-manic, bipolar depression
- tx bad taste
- tremor
- *** narrow therapeutic window
- *** diabetes insipidus
- *** hypothyroidism
- 10-21 day onset
- *** diuretics and NSAIDs increase blood lithium levels
- *** increased Na+ decreases lithium levels
- a benzo
- not much to note
Midazolam (Versed)
Flurazepam (Dalmane)
- long half life
- minimal tolerance
- *** can accumulate in elderly/ hepatic problems
- *** daytime sedation
Alprazolam (Xanax)
- benzo
- rapid oral absorp.
- short half-life and effects
- good for elderly
- tx for panic disorder, acute anxiety
d-Amphetamine (Adderall)
CNS stimulant for ADHD
- SSRI
- short half life
- *** withdrawal symptoms = flu-like/neurologic
- *** inhibits P450 (CYP2D6)
- mild sedation
Paroxetine (Paxil)
Venlafaxine (Effexor)
- SNRI
- ***HTN
- ***anxiety
- *** more rapid withdrawal symptoms
- nausea, somnolence, sweating, dizziness, sexual dysfunction
Phenytoin (Dilantin)
- 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