P3 Quiz 3 Flashcards
1
Q
Aripiprazole
A
Abilify
2
Q
Benztropine
A
Cogentin
3
Q
Carbamazepine
A
Tegretol, Carbatrol, Equetro
4
Q
Carbidopa with levodopa
A
Sinemet
5
Q
Desvenlafaxine
A
Pristiq
6
Q
Divalproex
A
Depakote
7
Q
Donepezil
A
Aricept
8
Q
Lamotrigine
A
Lamictal
9
Q
Levetiracetam
A
Keppra
10
Q
Lithium carbonate
A
Lithonate, Lithotabs, Lithobid
11
Q
Lurasidone
A
Latuda
12
Q
Memantine
A
Namenda
13
Q
Mirtazapine
A
Remeron
14
Q
Oxcarbazepine
A
Trileptal and Oxtellar XR
15
Q
Paroxetine
A
Paxil
16
Q
Phenobarbital
A
Phenobarbital
17
Q
Phenytoin
A
Dilantin Kapseals
18
Q
Quetiapine
A
Seroquel
19
Q
Pramipexole
A
Mirapex
20
Q
Risperidone
A
Risperdal
21
Q
Topiramate
A
Topamax
22
Q
Venlafaxine
A
Effexor
23
Q
Aripiprazole class
A
Antipsychotic
24
Q
Aripiprazole common FDA indications
A
Bipolar disorder, manic or mixed episodes, acute treatment: Adults, 10-15 mg po daily
Schizophrenia: Adults, 10-15 mg po daily
Depression, adjunctive with antidepressant: 2-4 mg po daily
Tourette syndrome: Children ≥6 y of age and <50 kg, 2 mg po daily, may titrate to 5-10 mg po daily; Children ≥6 y of age and ≥50 kg, 2 mg po daily, may titrate to 10-20 mg po daily
Irritability with autistic disorder: Children ≥6 y of age, 2 mg po daily × 7 d, then 5 mg po daily, may titrate to 15 mg/d
25
Aripiprazole MOA
Aripiprazole is an atypical antipsychotic agent (quinolinone derivative). It exhibits partial agonist activity at dopamine D2 and D3 receptors and serotonin 5-HT1A receptors and antagonist activity at 5-HT2A receptors.
26
Aripiprazole BBW
Dementia, suicidality
27
Aripiprazole DDI
CYP3A4/5 inducers- increase aripiprazole metabolism reduces aripiprazole efficacy
CYP3A4/5 , 2D6 inhibitors- decreased aripiprazole metabolism increases risk of aripiprazole toxicity
28
Aripiprazole common AE
Akathisia, anxiety, extrapyramidal effects, headache, increased appetite, somnolence, weight gain, hyperglycemia
29
Aripiprazole rare but serious AE
Slowed or difficult breathing when used in combination with opioids, compulsive behaviors, neuroleptic malignant syndrome, pancytopenia, QT prolongation, seizures, suicidal thoughts, tardive dyskinesia
30
Benztropine class
Antiparkinsonian, anticholinergic
31
Benztropine FDA indication
Extrapyramidal disease, medication-induced movement disorder: Adults, 1-4 mg po daily or bid
Parkinsonism: 1-2 mg/d po
32
Benztropine MOA
Benztropine possesses anticholinergic and antihistamine effects. May inhibit reuptake and storage of dopamine.
33
Benztropine MOA
Benztropine possesses anticholinergic and antihistamine effects. May inhibit reuptake and storage of dopamine.
34
Benztropine MOA
Benztropine possesses anticholinergic and antihistamine effects. May inhibit reuptake and storage of dopamine.
35
Benztropine MOA
Benztropine possesses anticholinergic and antihistamine effects. May inhibit reuptake and storage of dopamine.
36
Benztropine contraindications
Hypersensitivity to benztropine, patients <3 y of age
37
Benztropine DDI
Amantadine- Increased CNS toxicity
Phenothiazines- enhanced anticholinergic effects, decreased phenothiazine concentrations
Haloperidol- excessive anticholinergic effects
Thiazides- Anticholinergic agents may increase the serum concentration of thiazides
Potassium- anticholinergic agents may enhance the ulcerogenic effect of potassium
38
Benztropine common AE
Constipation, Nausea
39
Benztropine rare but serious AE
Anhidrosis, drug-induced psychosis, heat stroke, increased body temperature, tachycardia, visual hallucinations
40
Carbamazepine class
Anticonvulsant
41
Carbamazepine common FDA indications
Epilepsy, partial, generalized, and mixed types: Adults, 200 mg po bid, may titrate to 1200 mg po daily; Children <6 y of age, 10-20 mg/kg/d po in 2-4 divided doses, may titrate to 250-350 mg/d po (or 35 mg/kg/d); Children 6-12 y of age, 100 mg po bid, may titrate to 800 mg po daily
Trigeminal neuralgia: 100 mg po q12h, may titrate to 1200 mg po daily for pain control
42
Carbamazepine MOA
Carbamazepine acts presynaptically to block firing of action potentials, which decreases the release of excitatory neurotransmitters, and postsynaptically by blocking high-frequency repetitive discharge initiated at cell bodies.
43
Carbamazepine BBW
Agranulocytosis, aplastic anemia, dermatologic reactions (especially in asians), screen for HLA-B*1502
44
carbamazepine contraindications
Hypersensitivity to carbamazepine, history of bone marrow depression, MAOIs, nefazodone
45
Carbamazepine DDI
Acetaminophen- hepatotoxicity
CYP3A4/5 inducers- reduced carbamazepine efficacy
CYP3A4/5 inhibitors- decreased carbamazepine metabolism increases toxicity
CYP1A2, 2B6, 2C19, 2C8, 2C9, 3A4/5 and P-gb substrates- decreases substrate activity
Ergocalciferol- increased catabolism of vitamin D
Diuretics- increased risk of hyponatremia
Hormonal contraceptives- carbamazepine may render contraceptives less effective
MAOIs- increased risk of ergotism
Nefazodone- inhibit carbamazepine metabolism, induction of nefazodone metabolism
Warfarin- decreased anticoagulant efficacy
46
Carbamazepine common AE
Hyponatremia, dizziness, nausea
47
Carbamazepine rare but serious AE
Cardiac dysrhythmia, hepatitis, nephrotoxicity, pancreatitis, pancytopenia, Stevens-Johnson syndrome, syncope, toxic epidermal necrolysis, suicidal thoughts and behaviors
48
Carbidopa/levodopa class
Antiparkinsonian
49
Carbidopa/levodopa FDA indications
Parkinson disease: Immediate release, 25 mg/100 mg po tid, increasing dose to therapeutic response; extended release, 50 mg/200 mg po bid, separate doses by at least 6 h; extended-release capsules, 23.75 mg/95 mg po tid × 3 d, then may increase to 36.25 mg/145 mg po tid; patients generally treated with 400-1600 mg of levodopa per d; max 200 mg of carbidopa and 2000 mg of levodopa
50
Carbidopa/Levodopa MOA
When levodopa is administered orally, it is rapidly decarboxylated to dopamine in extracerebral tissues so that only a small portion of a given dose is transported unchanged to the CNS. For this reason, when given alone, large doses of levodopa are required for adequate therapeutic effect. However, these doses often result in nausea and other adverse reactions. Carbidopa inhibits decarboxylation of circulating levodopa, preventing nausea and allowing more levodopa to reach the CNS. Carbidopa does not cross the blood-brain barrier and does not affect the metabolism of levodopa within the CNS.
51
Carbidopa/levodopa contraindications
Hypersensitivity to carbidopa or levodopa, narrow-angle glaucoma, concurrent MAOI or linezolid
52
Carbidopa/levodopa DDI
D2 receptor antagonists (isoniazid, metoclopramide)- reduced therapeutic effect of levodopa
Linezolid- unknown, serotonin toxicity with severe HTN
MAOIs- severe HTN
Phenytoin, papaverine, iron salts- reversal of the effects of levodopa in Parkinson disease
Antihypertensive- risk of hypotension
53
Carbidopa/Levodopa common AE
Dyskinesia
54
Carbidopa/Levodopa rare but serious AE
Orthostatic hypotension, neuroleptic malignant syndrome, hallucinations, sleep attacks, compulsive behaviors
55
Desvenlafaxine class
SNRI
56
Desvenlafaxine FDA indications
Depression- 50 mg QD
57
Desvenlafaxine MOA
Desvenlafaxine is a potent reuptake inhibitor of serotonin and norepinephrine but lacks effects on muscarinic, α-adrenergic, or histamine receptors.
58
Desvenlafaxine BBW
Suicidality; not for use in children; not for bipolar disorder
59
Desvenlafaxine contraindications
Hypersensitivity to desvenlafaxine or venlafaxine; MAOI use
60
Desvenlafaxine DDI
Anticoagulants, antiplatelets, NSAIDs- increased risk of bleeding
Triptans, SSRIs, tramadol= increased risk of serotonin syndrome
Linezolid, metoclopramide, MAOI- increased risk of serotonin syndrome
61
Desvenlafaxine common AE
Diaphoresis, dizziness, headache, nausea, xerostomia
62
Desvenlafaxine rare but serious AE
GI hemorrhage, serotonin syndrome, suicidal thoughts
63
Divalproex class
Anticonvulsant
64
Divalproex common FDA indications
1. ) Absence seizure, simple and complex: 15 mg/kg/d po, may titrate to 60 mg/kg/d; delayed-release products are dosed bid, extended-release 24 h products are dosed daily
2. ) Complex partial epileptic seizure: 10-15 mg/kg/d po, may titrate to 60 mg/kg/d; delayed-release products are dosed bid, extended-release 24 h products are dosed daily
3. ) Manic bipolar disorder: 25 mg/kg/d po, may titrate to 60 mg/kg/d; delayed-release products are dosed bid, extended-release 24 h products are dosed daily
4. ) Migraine prophylaxis: Extended release 24 h, 500 mg po daily for 1 wk, then 1 g po daily; delayed release 250 mg po bid, increasing to 500 mg po bid
65
Divalproex MOA
Divalproex is composed of sodium valproate and valproic acid. Valproic acid is a carboxylic acid compound whose anticonvulsant activity might be mediated by an inhibitory neurotransmitter, GABA. Valproic acid might increase GABA levels by inhibiting GABA metabolism or enhancing postsynaptic GABA activity. Valproic acid also limits repetitive neuronal firing through voltage- and usage-dependent sodium channels.
66
Divalproex BBW
Hepatotoxicity, patients with mitochondrial disease, teratogenicity, pancreatitis
67
Divalproex Contraindications
Hypersensitivity to divalproex, hepatic disease, urea cycle disorders
68
Divalproex DDI
Aspirin, macrolides- increased valproic acid concentrations
Carbamazepine, ethosuximide, lamotrigine, rufinamide, TCAs- divalproex inhibits metabolism of these drugs, increasing toxicity
Acyclovir, carbapenems, protease inhibitors, rifampin, risperidone- decreased valproic acid conc and loss of anticonvulsants
Phenytoin, phenobarbital- altered levels of these and valproic acid levels
Olanzapine, oxcarbazepine- decreased olanzapine and oxcarbazepine concentrations
Warfarin- increased warfarin effect
Topiramate- increased hyperammonemia
69
Divalproex AE
Abdominal pain, alopecia, asthenia, diarrhea, diplopia, dizziness, headache, nausea, somnolence, tremor, vomiting
70
Divalproex rare but serious AE
Hepatitis, palpitation, pancreatitis, tachycardia, thrombocytopenia, suicidal ideation or behavior
71
Donepezil class
Central cholinesterase inhibitor
72
Donepezil common FDA indications
Alzheimer disease, dementia (mild-moderate): 5 mg po daily hs, may titrate to max 10 mg/d
Alzheimer disease, dementia (moderate-severe): 5 mg po daily qhs, may titrate to 10 mg/d at 4-6 wk to max 23 mg/d (immediate-release tablet) or 10 mg/d (disintegrating tablet)
73
Donepezil MOA
Donepezil enhances the action of acetylcholine by reversibly inhibiting acetylcholinesterase (AChE), the enzyme responsible for its hydrolysis. It has a high degree of selectivity for AChE in the CNS, which might explain the relative lack of peripheral side effects.
74
Donepezil DDI
Tolterodine, oxybutynin- decreased efficacy of donepezil
| Ramelteon- increased ramelteon exposure
75
Donepezil common AE
Asthenia
76
Donepezil rare but serious AE
Atrioventricular block, GI bleeding, torsades de pointes
77
Lamotrigine class
Phenyltriazine anticonvulsant
78
Lamotrigine common FDA indications
Bipolar I disorder: Adults 25 mg daily × 2 wk, then 50 mg po daily × 2 wk, then 100 mg po daily × 1 wk, then 200 mg po daily; may titrate to 400 mg po daily; regimens containing valproic acid, 25 mg po qod × 2 wk, then 25 mg po daily × 2 wk, then 50 mg po daily × 1 wk, then 100 mg po daily; regimens without valproic acid but containing carbamazepine, phenytoin, phenobarbital, primidone, rifampin, lopinavir/ritonavir: 50 mg po daily × 2 wk, then 50 mg po bid × 2 wk, then 100 mg po bid × 1 wk, then 300 mg/d po in divided doses × 1 wk, then 400 mg/d po in 2 divided doses
Partial seizure, adjunct or monotherapy, tonic-clonic seizure, Lennox-Gastaut syndrome, adjunctive: Adults and Children ≥12 y of age, immediate release, 100-500 mg/d po in 2 divided doses, extended release, 200-600 mg po daily; Children 2-12 y of age: immediate release, 1-15 mg/kg/d po in 1 or 2 divided doses, max 400 mg/d; dose initiation for combination regimens as noted above; dose titration required
79
Lamotrigine MOA
Lamotrigine is a phenyltriazine derivative unrelated to other marketed antiepileptic drugs (AEDs). Lamotrigine inhibits voltage-dependent sodium channels, thereby stabilizing neuronal membranes and reducing the release of excitatory neurotransmitters such as glutamate and aspartate.
80
Lamotrigine BBW
Serious skin reactions
81
Lamotrigine DDI
Enzyme inducers, rifampin, carbamazepine- decreased lamotrigine efficacy
Escitalopram- increased risk of myclonus
Estrogen based birth controls- decreased lamotrigine concentrations
Risperidone- increased risperidone concentrations
82
Lamotrigine common AE
Rash, ataxia, somnolence, headache, diplopia, rhinitis, nausea, vomiting, insomnia
83
Lamotrigine rare but serious AE
Stevens-Johnson syndrome, anemia, leukopenia, disseminated intravascular coagulation, thrombocytopenia, liver failure, aseptic meningitis, suicidal thoughts
84
Levetiracetam class
Anticonvulsant
85
Levetiracetam common FDA indications
1. ) Myoclonic seizure, adjunct: Children ≥12 y of age and Adults, initial, 500 mg po bid, titrate to target dose of 3000 mg/d
2. ) Partial seizure, adjunct: Children ≥16 y of age and Adults, immediate release, initial, 500 mg po bid, max 3000 mg/d; extended release, initial, 1000 mg po qd, max 3000 mg/d; Children 4-15 y of age, immediate release, initial, 10 mg/kg po bid, max 60 mg/kg/d; Children 6 mo to 3 y of age, initial 10 mg/kg po bid, max 50 mg/kg/d; Children 1-5 mo of age, 7 mg/kg po bid, max 42 mg/kg/d
3. ) Tonic-clonic seizure, primary generalized, adjunct: Children ≥16 y of age and Adults, initial, 500 mg po bid, titrate to target dose of 3000 mg/d; Children 6-15 y of age, initial, 10 mg/kg po bid, titrate to target dose of 60 mg/kg/d
86
Levetiracetam MOA
Levetiracetam is a pyrrolidine derivative that is structurally unrelated to other AEDs. Its mechanism of action is unclear and does not relate to any known mechanisms of neuronal excitation or inhibition. The action of levetiracetam in animal models of seizures and epilepsy is unique from other AEDs.
87
Levetiracetam DDI
Carbamazepine- increased carbamazepine toxicity
88
Levetiracetam common AE
Asthenia, fatigue, headache, somnolence, vomiting, increased BP
89
Levetiracetam rare but serious AE
Pancytopenia, hepatotoxicity, suicidal thoughts, suicide, Stevens-Johnson syndrome
90
Lithium class
Antimanic
91
Lithium common FDA indications
Bipolar disorder, maintenance therapy: Adults and Children >12 y of age, extended release, 900-1800 mg/d po in 2-3 divided doses; immediate release, initial 300 mg po daily, may titrate to 900-1800 mg po in 3-4 divided doses
Bipolar disorder, manic episode: Adults and Children >12 y of age, extended release, 1800 mg/d po in 2-3 divided doses; immediate release, 600 mg po tid
92
Lithium MOA
Lithium’s mechanism of antimanic effect is unknown; it alters the actions of several second-messenger systems (eg, adenylate cyclase and phosphoinositol). Alters cation transport across cell membrane in nerve and muscle cells and influences reuptake of serotonin and/or norepinephrine; second-messenger systems involving the phosphatidylinositol cycle are inhibited.
93
Lithium BBW
Lithium levels required
94
Lithium contraindications
Severe debilitation, dehydration, or sodium depletion; significant cardiovascular disease; significant renal impairment; concomitant diuretic therapy
95
Lithium DDI
Acetazolamide, sodium bicarbonate- decreased lithium conc
ACEIs, ARBs, diuretics, NSAIDs- increased risk of lithium toxicity
Agents that prolong QTc interval- additive cardiotoxicity
Antipsychotics drugs, clozapine- increased risk of AE and EPS
MAOIs- increased risk of malignant hyperpyrexia
SSRIs, linezolid- increased lithium concentrations and/or increased risk of serotonin syndrome
96
Lithium common AE
Cardiac dysrhythmias, fine tremor, hypothyroidism, leukocytosis, thrombocytosis, xerostomia
97
Lithium rare but serious AE
Hypotension, nephrotoxicity, seizure, hypercalcemia, hyperparathyroidism
98
Lurasidone class
Second generation (atypical) antipsychotics
99
Lurasidone common FDA label indication
Depressive episodes associated with bipolar disorder: Adults, 20 mg po daily, may titrate to max 120 mg po daily
Schizophrenia: Adults, 40 mg po daily, may titrate to max 160 mg/d
100
Lurasidone MOA
Lurasidone is an atypical antipsychotic agent (benzisothiazole-derivative). It exhibits relatively high affinity for dopamine D2 receptor and serotonin 5-HT7 and 5-HT2A receptors.
101
Lurasidone BBW
Dementia (increased mortality), suicidality
102
Lurasidone contraindications
Hypersensitivity, concurrent CYP3A4/5 inducers and inhibitors
103
Lurasidone DDI
CYP3A4/5 moderate inducers- increased lurasidone metabolism reduces efficacy
CYP3A4/5 inhibitors- decreased lurasidone metabolism increased risk of toxicity
104
Lurasidone common AE
Akathisia, extrapyramidal effects, headache, nausea, somnolence
105
Lurasidone rare but serious AE
Abnormal dreams, angioedema, bradycardia, neuroleptic malignancy syndrome, pancytopenia, seizures, suicidal thoughts, stroke, tardive dyskinesia
106
Memantine class
NMDA receptor antagonist
107
Memantine common FDA indication
Alzheimer disease: Immediate release, 5 mg po daily, may titrate dose no more than once per week to target dose of 10 mg po bid; extended release, 7 mg po daily, may titrate dose no more than once per week to target dose of 28 mg po daily
108
Memantine MOA
Activation of NMDA receptors by glutamate is believed to contribute to the symptomatology of Alzheimer disease. Memantine is believed to act as an uncompetitive (open-channel) NMDA receptor antagonist that binds preferentially to the NMDA receptor-operated cation channels. There is no evidence that memantine prevents or slows neurodegeneration in patients with Alzheimer disease.
109
Memantine DDI
Urinary alkalinizers- reduced memantine clearance
110
Memantine common AE
None known
111
Memantine rare but serious AE
Stevens-Johnson syndrome, DVT, hepatitis, liver failure, cerebrovascular accident, grand mal seizure, transient ischemic attack, acute renal failure
112
Mirtazapine class
antidepressant, alpha2 antagonist
113
Mirtazapine common FDA indications
Depression: 15 mg po daily hs, may titrate to response in 15 mg increments q1-2wk to 45 mg po daily hs
114
Mirtazapine BBW
Suicidality, not for use in children
115
Mirtazapine contraindications
Hypersensitivity to mirtazapine; concurrent use or use within 14 d of MAOI, linezolid, IV methylene blue use
116
Mirtazapine DDI
CYP2D6, 3A4/5, and 1A2 inducers- decreased mirtazapine efficacy
CYP2D6, 3A4/5, and 1A2 inhibitors- increased mirtazapine toxicity
Fluoxetine, fluvoxamine, linezolid, MAOIs, olanzapine, tramadol, venlafaxine- increased risk of serotonin syndrome
117
Mirtazapine common AE
Constipation, increased appetite, somnolence, xerostomia, increased serum cholesterol, weight gain
118
Mirtazapine rare but serious AE
Neutropenia, suicidal thoughts, QTc prolongation, torsades de pointes
119
Oxcarbazepine class
Dibenzapine carboxamide, anticonvulsant
120
Oxcarbazepine common FDA indication
Partial seizure: Adults, 300 mg po bid, may titrate to 1200-2400 mg/d po (depending on formulation); Children 4-16 y of age, 8-10 mg/kg/d po in 2 divided doses, may titrate to 600 mg/d po; Children <4 y of age and <20 kg, 16-20 mg/kg/d po in 2 divided doses, may titrate to a max 60 mg/kg/d
121
Oxcarbazepine DDI
CYP3A4/5 inducers- reduces oxcarbazepine efficacy
CYP3A4/5 inhibitors- increases oxcarbazepine toxicity
CYP3A4/5 substrates- decreases substrate concentration
CYP2C19 substrates- increase substrate activity
Carbamazepine, phenobarbital, valproic acid, verapamil- decreased oxcarbazepine concentrations
Oral contraceptives- decreased contraceptive efficacy
122
Oxcarbazepine common AE
Somnolence, HA, diplopia, dizziness
123
Oxcarbazepine rare but serious AE
Anaphylaxis, angioedema, Stevens-Johnson syndrome, suicidal thoughts, pancytopenia
124
Paroxetine class
SSRI
125
Paroxetine FDA indications
Depression: Adults, immediate release, 20 mg po daily, may titrate to 50 mg po daily; Adults, controlled release, 25 mg po daily, may titrate to 62.5 mg po daily; Children ≥8 y of age, 10-20 mg po daily
Generalized anxiety disorder: Adults, 20 mg po daily
Social anxiety disorder: Adults, 20 mg po daily; Children ≥8 y of age, 10 mg po daily
OCD: Adults, 20 mg po daily, may titrate to 60 mg po daily; Children ≥8 y of age, 10 mg po daily, may titrate to 30 mg daily
Panic disorder: Immediate release, 10 mg po daily, may titrate to 60 mg po daily; controlled release, 12.5 mg po daily, may titrate to 75 mg po daily
Posttraumatic stress disorder (PTSD): Adults, 20 mg po daily, may titrate to 50 mg po daily
Premenstrual syndrome: 12.5 mg po daily or × 14 d prior to expected start of menses, may titrate to 25 mg po daily
Vasomotor symptoms of menopause: 7.5 mg po daily at bedtime
126
Paroxetine BBW
Suicidality
127
Paroxetine contraindications
Hypersensitivity to paroxetine; concomitant use of thioridazine or MAOIs, pregnancy
128
Paroxetine DDI
CYP2D6 inhibitors- increases risk of paroxetine toxicity
Antiplatelet drugs, NSAIDs- increased risk of bleeding
Triptans, dextroamphetamine, tramadol, linezolid, MAOIs, opioids- increased risk of serotonin syndrome
Clozapine- increased clozapine conc
Agents that increase QTc interval- increased risk of QTc prolongation
129
Paroxetine common AE
Abnormal ejaculation, asthenia, constipation, diarrhea, headache, insomnia, nausea, somnolence
130
Paroxetine rare but serious AE
Serotonin syndrome, suicidal thoughts
131
Phenobarbital class
Long-acting barbiturate, C-IV
132
Phenobarbital common FDA indications
Epilepsy: Adults, 50-100 mg po bid-tid; Children, 15-50 mg po bid-tid (tablet) or 3-6 mg/kg/d po (solution)
Daytime sedation: Adults, 30-120 mg po divided into 2-3 doses, may titrate to 400 mg/d; Children, 6 mg/kg/d po divided into 3 doses
133
Phenobarbital MOA
Phenobarbital produces different degrees of depression within the CNS, from sedation to general anesthesia. It has been demonstrated to depress monosynaptic responses in the CNS only transiently, but synaptic recovery is delayed and a decrease in postsynaptic resistance is observed at some synapses.
134
Phenobarbital contraindications
Hypersensitivity to barbiturates; marked liver function impairment; respiratory disease with evidence of dyspnea or obstruction; history of sedative or hypnotic addiction; personal or family history of acute intermittent porphyria
135
Phenobarbital DDI
Substrates of CYP1A2, 2A6, 2B6, 2C8, 2C9, and 3A4/5- reduces substrate efficacy
CYP2C19 inducers- reduces phenobarbital efficacy
CYP2C19 inhibitors- increased phenobarbital toxicity
Barbiturates, benzodiazepines, opioids- additive CNS respiratory depression
Phenytoin- alter phenobarbital concentrations
Valproic acid- decreased valproic acid efficacy
136
Phenobarbital common AE
None Known
137
Phenobarbital rare but serious AE
Barbiturate withdrawal, bradyarrhythmia, megaloblastic anemia, respiratory depression, Stevens-Johnson syndrome
138
Phenytoin class
hydantoin anticonvulsant
139
Phenytoin common FDA indication
Seizure, generalized tonic-clonic, complex partial, or following neurosurgery, treatment, and prophylaxis: Adults, 100 mg po tid, may titrate to 200 mg po tid; doses up to 300 mg may be given once daily if capsule dosage form used; Children, 5 mg/kg/d po divided into 2-3 doses, may titrate to 300 mg/d
140
Phenytoin MOA
Phenytoin is a hydantoin that suppresses the spread of seizure activity mainly by inhibiting synaptic posttetanic potentiation and blocking the propagation of electric discharge. Phenytoin might decrease sodium transport and block calcium channels at the cellular level to produce these actions.
141
Phenytoin BBW
Hypotension and arrhythmias with IV administration
142
Phenytoin contraindications
Hypersensitivity to phenytoin, sinus bradycardia, AV block
143
Phenytoin DDI
CYP2C19, CYP2C9 inducers- reduces phenytoin efficacy
CYP2C19, CYP2C9 inhibitors- increases risk of phenytoin toxicity
Substrates of CYP2B6, 2C19, 2C8, 2C9, and 3A4/5- reduce efficacy of substrates
Acetaminophen- increased risk of hepatotoxicity
Carbamazepine, valproic acid- altered concentrations
144
Phenytoin common AE
gingival hyperplasia
145
Phenytoin rare but serious AE
Hepatotoxicity, pancytopenia, systemic lupus erythematosus, Stevens-Johnson syndrome, suicidal behavior, withdrawal seizures
146
Pramipexole class
Dopamine agonist, antiparkinson
147
Pramipexole common FDA indications
Parkinson disease: Immediate release, 0.125 mg po tid, may titrate to 0.5-1.5 mg po tid; ER, 0.375 mg po daily, may titrate to 4.5 mg po daily
Restless leg syndrome: Immediate release only, 0.125 mg po daily taken 2-3 h prior to bedtime, may titrate to 0.5 mg po daily
148
Pramipexole MOA
Pramipexole is a nonergot-derived dopamine subtype selective agonist that exerts activity in the CNS at D2 and D3 receptors but has no activity at the D1 receptor. D2 receptors are thought to play an important role in improving the akinesia, bradykinesia, rigidity, and gait disturbances of Parkinson disease.
149
Pramipexole DDI
Cimetidine-increased pramipexole concentrations
| Antipsychotics- may reduce the effectiveness of antipsychotic or dopamine agonist
150
Pramipexole common AE
Asthenia, dream disorder, dyskinesia, extrapyramidal movements, nausea, somnolence
151
Pramipexole rare but serious AE
Blackouts, heart failure, impulsive behavior, melanoma
152
Quetiapine class
Antipsychotic (atypical)
153
Quetiapine FDA indication
Bipolar disorder or schizophrenia, therapy initiation: Adults, immediate release, 50 mg po bid × 1 d, increase 50 mg/d × 3 d, may titrate to 800 mg/d; Adults, extended release, 300 mg po hs × 1 d, then 600 mg po hs × 1 d, may titrate to 800 mg/d; Children 10-17 y of age, immediate release, 50 mg po × 1 d, then 100 mg po × 1 d, then 200 mg po × 1 d, then 300 mg po × 1 d, then 400 mg po × 1 d, may titrate to 600 mg/d
Bipolar disorder or schizophrenia, maintenance: Adults, immediate release: 400-800 mg/d po; Adults, extended release, 400-800 mg/d po; Children 10-17 y of age, regular release, titrate to lowest effective dose
Major depressive disorder, adjunct to antidepressants: Adults, extended release, 50 mg po daily hs, may titrate to 300 mg/d
154
Quetiapine MOA
Quetiapine is an antagonist at multiple neurotransmitter receptors in the brain. It antagonizes serotonin 5-HT1A and 5-HT2, dopamine D1 and D2, histamine H1, and adrenergic α1 and α2 receptors. Efficacy in schizophrenia and bipolar disorder is due to the antagonism of a combination of D2 and 5-HT2 receptors.
155
Quetiapine BBW
Mortality in elderly with dementia, suicidality, not approved for children <10 y of age
156
Quetiapine DDI
CYP3A4/5 inducers- reduced quetiapine effectiveness
CYP3A4/5 inhibitors- increases quetiapine toxicity
Agents that prolong QTc interval- increased risk of QTc prolongation
157
Quetiapine common AE
Agitation, headache, HTN, somnolence, weight gain, xerostomia
158
Quetiapine rare but serious AE
Neuroleptic malignant syndrome, neutropenia, pancreatitis, sudden cardiac death, syncope, tardive dyskinesia, slowed or difficult breathing when used in combination with opioids
159
Risperidone class
Benzisoxazole, antipsychotic
160
Risperidone common FDA indications
Autistic disorder, irritability: Children ≥5 y of age and weighing <20 kg, 0.25 mg po daily, titrate to response; Children ≥5 y of age and weighing >20 kg, 0.5 mg po daily, titrate to response
Acute manic or mixed episodes of bipolar I disorder: Adults, 2-3 mg po daily, may titrate to 6 mg/d or 25-50 mg IM every 2 wk; Children ≥10 y of age, 0.5 mg po daily, may titrate to 6 mg/d
Schizophrenia: Adults, 1 mg po bid, may titrate to 18 mg/d or 25-50 mg IM every 2 wk; Children ≥13 y of age, 0.5 mg po daily, may titrate to 6 mg/d
161
Risperidone MOA
Risperidone is a potent serotonin-5-HT2 antagonist with weaker dopamine-D2 antagonism. Whereas typical antipsychotics are dopamine antagonists, the additional serotonin antagonism increases efficacy for negative symptoms of schizophrenia and reduces the likelihood of extrapyramidal symptoms.
162
Risperidone BBW
Mortality in elderly with dementia, DRESS
163
Risperidone contraindications
Hypersensitivity to risperidone, agents that increase QTc interval
164
Risperidone DDI
CYP2D6, P-glycoprotein inhibitors- increases toxicity
P-glycoprotein inducers- reduces risperidone efficacy
Agents that prolong QTc interval
Valproic acid- increased valproic acid concentrations
Anticholinergics- additive anticholinergic activity
165
Risperidone common AE
Extrapyramidal symptoms, insomnia, anxiety, fatigue, metabolic changes (hyperglycemia, dyslipidemia, weight gain, DM)
166
Risperidone rare but serious AE
Neuroleptic malignant syndrome, pancreatitis, stroke, pancytopenia, sudden cardiac death, syncope, tardive dyskinesia, priapism, slowed or difficult breathing when used in combination with opioids, seizure, suicidal ideation or behavior
167
Topiramate class
Anticonvulsant
168
Topiramate common FDA indication
Partial or tonic-clonic seizure, monotherapy or adjunct: Children 2-16 y of age, 1-3 mg/kg/d (max 25 mg) po daily × 1 wk, may titrate to 5-9 mg/kg/d; Children ≥17 y of age and Adults, 25 mg po bid × 1 wk, may titrate to max of 200 mg po bid
Migraine prophylaxis: Immediate release only, initial 25 mg po daily × 1 wk, may titrate to max of 50 mg po bid
169
Topiramate MOA
The exact mechanisms by which topiramate exerts its anticonvulsant and migraine prophylaxis effects are unknown. Electrophysiologic and biochemical evidence suggests that topiramate blocks voltage-dependent sodium channels, augments the activity of the neurotransmitter gamma-aminobutyrate at some subtypes of the GABA-A receptor, antagonizes the AMPA/kainate subtype of the glutamate receptor, and inhibits the carbonic anhydrase enzyme, particularly isozymes II and IV.
170
Topiramate contraindications
Hypersensitivity, alcohol use for the ER formulation (within 6 h prior to and 6 h after administration)
171
Topiramate DDI
Amitriptyline- may increase amitriptyline concentrations
Oral contraceptives- reduces contraceptive efficacy
CNS depressants- additive CNS derpression
172
Topiramate common AE
Ataxia, loss of appetite, dizziness, impaired psychomotor performance, somnolence, fatigue, nystagmus, low serum bicarbonate
173
Topiramate rare but serious AE
Erythema multiforme, Stevens-Johnson syndrome, hypohidrosis, increased body temperature, metabolic acidosis, liver failure, glaucoma, myopia, suicidal ideation, visual field defects
174
Venlafaxine class
antidepressant, SNRI
175
Venlafaxine common FDA indication
Generalized anxiety disorder: Extended release, 37.5-75 mg po daily, may titrate to 225 mg/d
Depression: Immediate release, 37.5-75 mg po daily in 2-3 divided doses, may titrate to 375 mg/d; extended release, 37.5-75 mg po daily, may titrate to 375 mg/d
Panic disorder: Extended release, 37.5 mg po daily × 7 d, then 75 mg po daily, then may titrate to 225 mg/d
Social anxiety disorder: Extended release, 37.5 mg po daily, may titrate to 75 mg po daily
176
Venlafaxine MOA
Potent reuptake inhibitor of serotonin and norepinephrine but lacks effects on muscarinic, α-adrenergic, or histamine receptors.
177
Venlafaxine BBW
Suicidal ideation
178
Venlafaxine contraindications
Hypersensitivity, MAOIs
179
Venlafaxine DDI
Agents that prolong QTc interval
Anticoagulants, antiplatelets, NSAIDs
CYP3A4/5, 2D6 inhibitors- increased venlafaxine tox
CYP3A4/5 inducers- reduces venlafaxine efficacy
Dextroamphetamine, SSRIs, SNRIs, sumatriptan, tramadol, trazodone, zolmitriptan, MAOIs- increased risk of serotonin syndrome
180
Venlafaxine common AE
Dizziness, headache, insomnia, nausea, somnolence, xerostomia, weakness
181
Venlafaxine rare but serious AE
GI hemorrhage, hepatotoxicity, serotonin syndrome, suicidal thoughts
