Drugs to know Flashcards
(106 cards)
1
Q
- CNS stimulant
- agonist at nicotinic neuronal receptor
- some people have a gene that impairs metabolism, protecting them addiction
- use common in schizo
A
Nicotine
2
Q
- 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
A
Diazepam (Valium)
3
Q
- 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
A
Phenytoin (Dilantin)
4
Q
Methylphenidate (Ritalin)
A
- CNS stimulant for ADHD
5
Q
Divalproex (Depakote)
A
- anti-mania
- rapid loading
- a lot like valproic acid
6
Q
Amitriptyline (Elavil)
A
- 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
7
Q
Diazepam (Valium)
A
- 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
8
Q
- antagonist at the benzodiazepine binding site –> reverse CNS effects of benzos (OD or for to hasten surgery recovery)
A
Flumazenil (Romazicon)
9
Q
- 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
A
Trazodone (Desyrel)
10
Q
- atypical antipsychotic
- tx of negative symptoms
- ***agranulocytosis
- ***hypersalivation
- *** lowers sz threshold
- weight gain
- try other drugs first!
A
Clozapine (Clozaril)
11
Q
Ramelteon (Rozerem)
A
- Agonist at melatonin MT1 and MT2 (superchiasmatic nucleus of the thalamus)
- induces sleep and regulates circadian rhythms
12
Q
Nitrous oxide
A
- inorganic gas (volatile) inhaled general anesthetic
- low potency (MAC = 105%)
- adjunctive agent
- analgesic and anxiolytic
- rapid onset and recovery
13
Q
Heroin
A
- Opioid agonist
- Naltrexone (Revia) and Buprenorphine (Subutex) block reinforcing effects but don’t change cravings
- death by respiratory depression
14
Q
Carbamazepine (Tegretol)
A
- 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
15
Q
Phenobarbital (Luminal)
A
- 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
16
Q
Clozapine (Clozaril)
A
- atypical antipsychotic
- tx of negative symptoms
- ***agranulocytosis
- ***hypersalivation
- weight gain
- try other drugs first!
17
Q
- atypical antipsychotic
- ***best tx for bipolar depression
- sedation
- weight gain
A
Quetiapine (Seroquel)
18
Q
- 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
A
Phenobarbital (Luminal)
19
Q
- 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
A
Levetiracetam (Keppra)
20
Q
- 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
A
Amitriptyline (Elavil)
21
Q
- blocks T-type Ca++ channels
- *** first line for absence sz c
- omplete metabolism by CYP3A4
- gastric distress
- HA
- dizziness
- gum hypertrophy
A
Ethosuximide (Zarontin)
22
Q
- benzo
- long half life
- minimal tolerance
- *** can accumulate in elderly/ hepatic problems
- *** daytime sedation
A
Flurazepam (Dalmane)
23
Q
Escitralopram (Lexapro)
A
- SSRI
- no sedation
24
Q
- 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
A
Marijuana
25
Methamphetamine
* CNS stimulant
* acts upon locus ceruleus
* increases NE release
* reverses DA transporter to release DA
* makes schizo worse
26
* SSRI
* no sedation
Escitralopram (Lexapro)
27
* NMDA antagonist
* dissociative anesthetic- IV
* allows responsivity and reflexes with catatonia, amnesia, and analgesia, esp. in kids
* worsens schizo
ketamine
28
* 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
29
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
30
* benzo
* short half-life
* less daytime sedation but + rebound insomnia
* rapid oral
* anterograde amnesia
* confusion
* bizzare behavior
* agitation
* hallucinations
Triazolam (Halcion)
31
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)
32
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
33
* Agonist at melatonin MT1 and MT2 (superchiasmatic nucleus of the thalamus)
* induces sleep and regulates circadian rhythms
Ramelteon (Rozerem)
34
* typical antipsychotic
* low potency
* less EPS but high ANS SEs:
* anti-M (dry mouth, sedation)
* α1-blockade (hypotension)
* antihistamine (sedation)
Chlorpromazine (Thorazine)
35
* CNS stimulant
* acts upon locus ceruleus
* increases NE release
* reverses DA transporter to release DA
* makes schizo worse
Methamphetamine
36
Flumazenil (Romazicon)
* antagonist at the benzodiazepine binding site --\> reverse CNS effects of benzos (OD or for to hasten surgery recovery)
37
* SSRI
* \*\*\* inhibits P450 (CYP2D6)
* longer half life
* mild sedation
Fluoxetine (Prozac)
38
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
39
Fluoxetine (Prozac)
* SSRI
* \*\*\* inhibits P450 (CYP2D6)
* longer half life
* mild sedation
40
* partial agonist at mu opioid receptor
* blocks reinforcing effects of heroin
* no ups and downs
* lose cravings
Buprenorphine (Subutex)
41
Cocaine
* CNS stimulant
* blocks DA reuptake (and possibly 5HT, NE)
* makes schizo worse
42
Buprenorphine (Subutex)
* partial agonist at mu opioid receptor
* blocks reinforcing effects of heroin
* no ups and downs
* lose cravings
43
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
44
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
45
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
46
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
47
Amphetamines
* CNS stimulant
* acts upon locus ceruleus
* increases NE release
* reverses DA transporter to release DA
* makes schizo worse
48
Triazolam (Halcion)
* benzo
* short half-life
* less daytime sedation but + rebound insomnia
* rapid oral
* anterograde amnesia
* confusion bizzare
* behavior
* agitation
* hallucination
49
* 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
50
* 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
51
* 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)
52
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)
53
Midazolam (Versed)
* benzo
* not much to note
54
Methadone
* long acting opioid agonist
* substitute for heroin to alleviate symptoms (no ups and downs, lose cravings)
55
* 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)
56
* benzo
* slow oral absorp.
* intermediate half life
* less depression of REM sleep
Temazepam (Restoril)
57
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
58
Haloperidol (Haldol)
* typical antipsychotic
* high potency
* tx of positive symptoms
* \*\*\*high EPS SEs (dystonia, akathisia, pseudoparkinsons, tardive dyskinesias)
59
CNS stimulant for ADHD
Methylphenidate (Ritalin)
60
* 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)
61
Temazepam (Restoril)
* benzo
* slow oral absorp.
* intermediate half life
* less depression of REM sleep
62
* 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)
63
* 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)
64
* anti-mania
* rapid loading
* a lot like valproic acid
Divalproex (Depakote)
65
ketamine
* NMDA antagonist
* dissociative anesthetic- IV route
* allows responsivity and reflexes with catatonia, amnesia, and analgesia, esp. in kids
* worsens schizo
66
Nicotine
* CNS stimulant
* agonist at nicotinic neuronal receptor
* some people have a gene that impairs metabolism, protecting them from addiction
* use common in schizo
67
* 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)
68
Oxazepam (Serax)
* benzo
* direct metabolism (no P450)
* short half life
* \*\*\* good for elderly and hepatic dysfunction
* slow oral absorp.
69
* 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)
70
* antagonist at Histamine H1 and muscarinic cholinergic receptors
* sedation
* antimuscarinic in elderly
* \*\*\* treatment for acute dystonia (an EPS)
Diphenhydramine (Benadryl)
71
Disulfiram (Antabuse)
* inhibits aldehyde dehydrogenase (AIDH)
* causes 5-10x fold increase in acetaldehyde levels --\> nausea/vomiting, respiratory and cardiovascular collapse, convulsions
72
* benzo
* direct metabolism (no P450)
* short half life
* \*\*\* good for elderly and hepatic dysfunction
* slow oral absorp.
Oxazepam (Serax)
73
* SNRI
* \*\*\*HTN
* \*\*\*anxiety
* \*\*\* more rapid withdrawal symptoms
* nausea, somnolence, sweating, dizziness, sexual dysfunction
Venlafaxine (Effexor)
74
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
75
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
76
* benzo
* rapid oral absorp.
* short half-life and effects
* good for elderly
* tx for panic disorder, acute anxiety
Alprazolam (Xanax)
77
Quetiapine (Seroquel)
* atypical antipsychotic
* \*\*\*best tx for bipolar depression
* sedation
* weight gain
78
* 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
79
* 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)
80
Ethosuximide (Zarontin)
* blocks T-type Ca++ channels
* \*\*\* first line for absence sz
* complete metabolism by CYP3A4
* gastric distress, HA, dizziness, gum hypertrophy
81
Paroxetine (Paxil)
* SSRI
* short half life
* \*\*\* withdrawal symptoms = flu-like/neurologic
* \*\*\* inhibits P450 (CYP2D6)
* mild sedation
82
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
83
* inhibits aldehyde dehydrogenase (AIDH)
* causes 5-10x fold increase in acetaldehyde levels --\> nausea/vomiting, respiratory and cardiovascular collapse, convulsions
Disulfiram (Antabuse)
84
* CNS stimulant
* blocks DA reuptake (and possibly 5HT, NE)
* makes schizo worse
Cocaine
85
* 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)
86
Diphenhydramine (Benadryl)
* antagonist at Histamine H1 and muscarinic cholinergic receptors
* sedation
* antimuscarinic in elderly
* \*\*\* treatment for acute dystonia (EPS)
87
* long acting opioid agonist
* substitute for heroin to alleviate symptoms (no ups and downs, lose cravings)
Methadone
88
* 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
89
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
90
* 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)
91
* inorganic gas (volatile)
* inhaled general anesthetic
* low potency (MAC = 105%)
* adjunctive agent
* analgesic and anxiolytic
* rapid onset and recovery
Nitrous oxide
92
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
93
* CNS stimulant
* acts upon locus ceruleus
* increases NE release
* reverses DA transporter to release DA
* makes schizo worse
Amphetamines
94
* typical antipsychotic
* high potency
* tx of positive symptoms
* \*\*\*high EPS SEs (dystonia, akathisia, pseudoparkinsons, tardive dyskinesias)
Haloperidol (Haldol)
95
* Opioid agonist
* Naltrexone (Revia) and Buprenorphine (Subutex) block reinforcing effects but don't change cravings
* death by respiratory depression
Heroin
96
CNS stimulant for ADHD
d-Amphetamine (Adderall)
97
Chlorpromazine (Thorazine)
* typical antipsychotic
* low potency
* less EPS but high ANS SEs:
* anti-M (dry mouth, sedation)
* α1-blockade (hypotension)
* antihistamine (sedation)
98
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
99
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
100
* a benzo
* not much to note
Midazolam (Versed)
101
Flurazepam (Dalmane)
* long half life
* minimal tolerance
* \*\*\* can accumulate in elderly/ hepatic problems
* \*\*\* daytime sedation
102
Alprazolam (Xanax)
* benzo
* rapid oral absorp.
* short half-life and effects
* good for elderly
* tx for panic disorder, acute anxiety
103
d-Amphetamine (Adderall)
CNS stimulant for ADHD
104
* SSRI
* short half life
* \*\*\* withdrawal symptoms = flu-like/neurologic
* \*\*\* inhibits P450 (CYP2D6)
* mild sedation
Paroxetine (Paxil)
105
Venlafaxine (Effexor)
* SNRI
* \*\*\*HTN
* \*\*\*anxiety
* \*\*\* more rapid withdrawal symptoms
* nausea, somnolence, sweating, dizziness, sexual dysfunction
106
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