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Clinical Pharmacology of SSRI's
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(Page numbers in italics indicate figures;
page numbers followed by "t" indicate tables.)
Acetaminophen, 159t
Acetylcholine receptor blockade
consequences of, 48t
tricyclic antidepressants and, 67
Age, SSRI clearance rate and, 120t-121t,
124-125
Alcohol, antidepressant interaction with, 65-66
Alfentanil, 159t
a-Adrenergic receptor blockade, 49t
Alprazolam
CYP enzyme metabolism of, 159t
drug interactions with, 190-192,
193t
Alprenolol, 158t
Amidarone, 159t
Amitriptyline
CYP enzyme metabolism of, 158t-159t
dopamine uptake and, 39t
norepinephrine uptake and, 38t,
41
polypharmacy of, 25t
potency of, 27
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
side effects of, 70
Analgesic(s), 159t
Androstendione, 159t
Anesthetic(s), local, 159t
Anorexia
imipramine and, 68t
serotonin uptake blockade and, 48t
SSRIs and, 82t,
86t, 87
Antiarrhythmic drug(s)
CYP enzyme metabolism of, 158t-159t
drug interactions with, 184
Antibiotic(s), 159t
Anticonvulsant drug(s), 159t
Antidepressant(s). See also specific drug, eg, Fluoxetine; specific
type of drug, eg, Monoamine oxidase inhibitor(s).
action mechanisms of, 16t
CYP enzyme metabolism of, 158t-159t
pharmacology of, 48t-49t
prevalence of other drugs with, prevalence
of, 162t
side effects of, 48t-49t
in vitro profile of, 53
Antiestrogen drug(s), 159t
Antihistamine(s), 159t
Antipsychotic drug(s), 158t-159t
Anxiety
amitriptyline and, 70
serotonin uptake blockade and, 48t
sertraline and, 70
SSRIs and, 86t
Astemizole
CYP enzyme metabolism of, 159t
drug interactions with, 153t
Asthenia
serotonin uptake blockade and, 48t
SSRIs and, 86t
Barbiturate(s), 158t
Benzodiazepine(s)
CYP enzyme metabolism of, 159t
development of, 20
SSRI(s) interaction with, 66
Benzphetamine, 159t
Benztropine, 25t
ß-Blocker(s)
CYP enzyme metabolism of, 158t
drug interactions with, 184
Bupropion
fluoxetine interaction with, 150
seizure risk with, 149,
150
Burarolol, 158t
Caffeine, 158t
Calcium channel blocker(s), 159t
Carbamazepine
CYP enzyme metabolism of, 159t
drug interactions with, 152t,
156, 192,
193t
Carcinogenesis, CYP enzyme 2D6 and, 138-140
Central depressant drug(s), histamine receptor blockade and,
48t
Chirality, 29-32
Cimetidine
action mechanism of, 25t
drug interactions with, 152t
Cisapride, 159t
Citalopram. See also Desmethylcitalopram.
availability of, 18
brand names of, by country, 234t-236t
chirality of, 30-31
clearance of, age and gender and, 120t,
124-125
CYP enzymes and, 176t-177t
2D6 deficiency and, 165t
2D6 functions and, 179t,
185, 186
inhibition by, 170t-171t
metabolism of, 158t
development of, 16
dopamine uptake and, 39t
dosage of
age and, plasma level
and, 120t
potency and, 50t,
51-52
half-life of, 60t,
109t, 118t,
119
cirrhosis and, 127t
metabolism of, 110-111,
111t
metabolites of, potency of, 57,
58t
norepinephrine uptake and, 38t,
41
pharmacokinetics of, 109t
linear versus nonlinear,
117-119
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
dosage and, 50t,
51-52
steady-state of, time to, 123
structural formula of, 17
in vitro profile of, 53
washout of, 123
Citalopram enantiomer(s), 44t
Clarithromycin, 159t
Clomipramine. See also Desmethylclomipramine.
action mechanisms of, 52,
54
CYP enzyme metabolism of, 158t,
159t
demethylation of, 55
potency and, 56
dopamine uptake and, 39t
half-life of, 60t
for major depression, 54
norepinephrine uptake and, 38t,
41
for obsessive-compulsive disorder, 54
selectivity of, 46t
side effects and, 54
selectivity ratio of, 41
serotonin uptake and, 37t,
41
sodium channel inhibition by, 54
in vitro profile of, 53
Clonazepam, 159t
Clonidine
adrenergic blocker interaction with, 49t
antidepressant interaction with, 49t
Clorpheniramine, action mechanism of, 25t
Clozapine
CYP enzyme metabolism of, 158t,
159t
seizure risk with, 148,
149
Cocaine, 159t
Codeine
CYP enzyme metabolism of, 158t,
159t
drug interactions with, 153t,
184
Constipation
acetylcholine receptor blockade and, 48t
amitriptyline and, 70
imipramine and, 68,
68t
sertraline and, 70
SSRIs and, 83t,
86t
Cortisol, 159t
Cyclosporine, 159t
CYP enzyme(s)
antidepressant demethylation and, 55-56
citalopram metabolism by, 110-111,
111t
classification of, 132-133,
134t
clozapine metabolism by, 150
deficiency of, 138-140
genetically determined,
160t
discovery of, 131t,
131-132, 133t
drug clearance and, 140-141,
141-142, 143
drug metabolism by, 135,
136, 137
drug-drug interactions and, 143-144,
152t-153t
fluoxetine metabolism by, 111t,
111-113
fluvoxamine metabolism by, 111t,
111-112
functions of, 136t,
138
genetics of, 134t,
137
inhibition constant and, 227-232
inhibition of
consequences of, 163,
164t
in vitro studies
of, 167t, 167-169,
170t-171t
in vivo studies
of, 167t, 172,
173, 174-175
norfluoxetine inhibition of, 59
oxidative metabolism and, 137,
139
paroxetine metabolism by, 111t,
113-114
reaction cycle of, 138
risperidone metabolism by, 148
sertraline metabolism by, 111t,
114-115
SSRI inhibition of, 78,
98
steroidogenic, 133,
134t, 135,
136t
tricyclic antidepressant metabolism by,
151
xenobiotic, 134t,
135, 136t,
175, 176t-177t,
178
CYP enzyme 1A2
drugs metabolized by, 158t
effects of specific SSRIs on, 176t-177t,
178, 180-181
CYP enzyme 2C9/10
drugs metabolized by, 158t
effects of specific SSRIs on, 176t-177t,
181-182, 193t
CYP enzyme 2C19, effects of specific SSRIs on, 176t-177t,
182-183, 193t
CYP enzyme 2D6
carcinogenesis and, 138-140
deficiency of, drug-induced, 163
dopamine uptake transporter pump and, 137
drugs metabolized by, 158t
effects of specific SSRIs on, 176t-177t,
179t-180t, 184,
185, 186-187,
190, 230t
myths concerning, 164,
166, 166t
tricyclic antidepressant toxicity and, 100-101
CYP enzyme 3A3/4
drugs metabolized by, 159t
effects of specific SSRIs on, 176t-177t,
190-192, 193t,
194
Cytochrome P450 enzyme(s). See CYP enzyme(s).
Dapsone, 159t
Debrisoquin, 158t
Dehydroepiandrosterone 3-sulfate, 159t
Depression, major
clomipramine for, 54
prevalence of medical illnesses with, 162t
SSRI(s) for, 75t
tricyclic antidepressants for, 72
Desipramine
action mechanism of, 25t
CYP 2D6 functions and, 186,
188-189
dopamine uptake and, 39t
drug interactions with, 173,
186, 188-189
norepinephrine uptake and, 38t,
41
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
Desmethylcitalopram
CYP enzymes and
inhibition by, 170t-171t
metabolism of, 158t
potency of, 58t,
60t
Desmethylclomipramine
clinical relevance of, 60t
CYP enzyme metabolism of, 158t
half-life of, 60t
potency of, 44t,
58t
selectivity of, 41
in vitro profile of, 53
Desmethylsertraline
CYP enzymes and, 115
inhibition by, 170t-171t
pharmacokinetics of, 116-117
potency of, 58t
Desmethylvenlafaxine, 159t
Dexamethasone, 159t
Dextromethorphan
CYP enzyme metabolism of, 158t,
159t
drug interactions with, 152t
Diabetes mellitus, depression prevalence with, 162t
Diarrhea
amitriptyline and, 70
imipramine and, 68t
serotonin uptake blockade and, 48t
sertraline and, 70
SSRIs and, 82t,
86t
Diazepam
CYP enzyme metabolism of, 159t
drug interactions with, 182-183
Diltiazem, 159t
Disopyramide, 159t
drug interactions with, 152t
Dizziness
amitriptyline and, 70
imipramine and, 68t
sertraline and, 70
SSRIs and, 48t,
82t, 86t
Docetaxel, 159t
Dopamine uptake
antidepressant potency and, 39t,
40
drug selectivity and, 44t-45t
SSRI metabolites and, 57,
58t, 60t
Drowsiness
histamine receptor blockade and, 48t
imipramine and, 68t
SSRIs and, 82t,
86t, 87
Drug development. See also specific drug, eg, Lithium,
development of.
criteria for, 19t
mechanism of action in, 18-19,
19t, 21
molecular targeting in, 21
signal-to-noise ratio in, 24
site of action in, 18-20,
19
Drug interaction(s). See also specific drug, eg, Monoamine
oxidase inhibitor(s), SSRI interaction with.
clearance rate and, 145-146
CYP enzymes and, 143-144,
152t-153t
pharmacodynamic, 144-145,
145t
pharmacokinetic, 145,
145t-146t, 150
CYP enzymes and, 155-157,
156, 160
studies of, 173
Drug monitoring. See Therapeutic drug monitoring.
Drug potency
concentration and, 43,
47, 50t,
51-52
determination of, 33-35,
35
Dry mouth
acetylcholine receptor blockade and, 48t
amitriptyline and, 70
imipramine and, 68,
68t
sertraline and, 70
SSRIs and, 82t,
86t
Dyspepsia, SSRIs and, 82t
Ejaculation, premature, SSRIs for, 91
Enantiomer. See also specific drug, eg, Citalopram enantiomer(s).
definition of, 29-30
drug monitoring and, 30
pharmacokinetics of, 30
Encainide, 158t
Epilepsy, depression prevalence with, 162t
Erythromycin
CYP enzyme metabolism of, 159t
drug interactions with, 152t,
155
Estradiol, 159t
Ethosuximide, 159t
Ethylmorphine, 158t
Fatigue
amitriptyline and, 70
imipramine and, 68t
sertraline and, 70
SSRIs and, 82t,
86t, 87
Felodipine, 159t
Fenfluramine, 48t
Flecainide, 158t
Fluoxetine. See also Norfluoxetine.
availability of, 18
benzodiazepine interaction with, 66
brand names of, by country, 234t-236t
bupropion interaction with, 150
chirality of, 31
clearance of, age and gender and, 120t,
124-125
CYP enzymes and
2C9/10 and, 193t
2C19 and, 193t
2D6 and, 179t-180t,
185, 186,
230t
2D6 deficiency and, 163,
165t
3A3/4 and, 193t
inhibition by, 170t-171t
metabolism of, 158t
development of, 16
dopamine uptake and, 39t
dosage of
age and, plasma level
and, 120t
efficacy and, 85
potency and, 50t,
51-52
drug interactions with, 152t,
181, 182-184,
188
effects of, on specific CYP enzymes, 176t-177t
efficacy of, acute, 92t,
93-95
half-life of, 60t,
109t, 118t,
119-123
cirrhosis and, 127t
metabolism of, 111t,
111-113
metabolites of, 116
potency of, 57,
58t, 59
norepinephrine uptake and, 38t,
41
pharmacokinetics of, 109t
linear versus nonlinear,
117-119
relapse rate with, 92t,
97-98
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
dosage and, 50t,
51-52
side effects of
discontinuation rate from,
84
incidence of, 82t-83t,
86t
steady-state of, time to, 123
structural formula of, 17
in vitro profile of, 53
washout of, 80,
123
Fluoxetine enantiomer(s), 45t
Fluvoxamine
availability of, 18
benzodiazepine interaction with, 66
brand names of, by country, 234t-236t
clearance of, age and gender and, 120t,
124-125
CYP enzymes and
1A2 and, 178
2C9/10 and, 193t
2C19 and, 193t
2D6 and, 179t,
185, 230t
2D6 deficiency and, 165t
3A3/4 and, 193t
inhibition by, 170t-171t
development of, 16
dopamine uptake and, 39t
dosage of
age and, plasma level
and, 120t
potency and, 50t,
51-52
drug interactions with, 152t,
155, 178-179,
182-183, 190-192
effects of, on specific CYP enzymes, 176t-177t
efficacy of, acute, 92t,
93-94
half-life of, 60t,
109t, 118t,
123
cirrhosis and, 127t
metabolism of, 111t,
111-112
norepinephrine uptake and, 38t,
41
for obsessive-compulsive disorder, 18
pharmacokinetics of, 109t
linear versus nonlinear,
117-119
relapse rate with, 92t,
98-99
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
dosage and, 50t,
51-52
side effects of, incidence of, 82t-83t,
86t
steady-state of, time to, 123
structural formula of, 17
in vitro profile of, 53
washout of, 123
withdrawal from, 122-123
Gender, SSRI clearance rate and, 120t-121t,
124-125
Guanabenz, adrenergic blocker interaction with, 49t
Guanethidine, antidepressant interaction with, 48t
Guillain-Barré syndrome, as SSRI side effect, 16
Haloperidol, 158t
Headache
imipramine and, 68t
SSRIs and, 48t,
82t, 86t
Heart
acetylcholine receptor blockade and, 48t
SSRIs and
tricyclic antidepressant effects on, 55,
67, 74
Heart disease
depression prevalence with, 162t
SSRI metabolism and, 125,
128
Hexobarbital, 158t
Histamine receptor blockade, 48t,
54
Hydroamphetamine, 158t
Hypertension drug(s), antidepressant interaction with, 48t-49t,
66-67
Hypotension, adrenergic blockade and, 49t
Imipramine
CYP enzyme metabolism of, 158t,
159t
dopamine uptake and, 39t
norepinephrine uptake and, 38t,
41
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
side effects of, 68t,
69
Immunosuppressant drug(s), 159t
Inhibition constant, CYP enzyme effects and, 227-232
Insomnia
amitriptyline and, 70
imipramine and, 68t
serotonin uptake blockade and, 48t
sertraline and, 70
SSRIs and, 82t
Jitteriness, norepinephrine uptake blockade and, 48t
Ketoconazole, drug interactions with, 153t,
155
Lidocaine, 158t-159t
Lithium
development of, 20
SSRI interaction with, 48t
Liver disease, SSRI metabolism and, 125-126,
127t
Loratadine, 159t
Lovastatin, 159t
Macrolide antibiotic(s), 159t
Mechanism of action. See also specific drug, eg, Fluoxetine,
action mechanism of.
definition of, 18-19,
19t
Memory impairment, acetylcholine receptor blockade and, 48t
Menstrual disorder, SSRIs and, 88t
Mephenytoin, 158t
Mephobarbital, 158t
Metoprolol, 158t
Mexiletine, 158t
Midazolam, 159t
Migraine, SSRIs and, 48t
Minodipine, 159t
Molecular targeting, in drug development, 21
Monoamine oxidase inhibitor(s)
action mechanisms of, 16t,
22, 23
development of, 20-21
evolution of, 22
SSRI interaction with, 48t,
79-80, 144-145
Muscarinic acetylcholine receptor blockade
consequences of, 48t
tricyclic antidepressants and, 67
Myocardial infarction, depression prevalence with, 162t
Nausea
amitriptyline and, 70
imipramine and, 68t
serotonin uptake blockade and, 48t
sertraline and, 70
SSRIs and, 69,
82t, 86t
Nefazodone. See Phenylpiperazine (Nefazodone).
Nervousness
imipramine and, 68t
SSRIs and, 82t,
86t, 87
Neuroleptic drug(s), drug interactions with, 184
Nicardipine, 159t
Nifedipine, 159t
Niludipine, 159t
Nisoldipine, 159t
Nitrendipine, 159t
Norepinephrine inhibitor(s), examples of, 16t
Norepinephrine uptake
antidepressant potency and, 38t,
40, 41
blockade of, consequences of, 48t
drug selectivity and, 42,
44t-45t
SSRI metabolites and, 57,
58t, 60t
Norfluoxetine
biogenic amine uptake and, 45t
chirality of, 31
CYP 2D6 functions and, 180t
CYP enzyme inhibition by, 59,
170t-171t
drug interactions with, 155,
184, 188,
190-192
half-life of, 60t,
119
cirrhosis and, 127t
pharmacokinetics of, 116
potency of, 58t,
60t
steady-state of, time to, 123
washout of, 123
Nortriptyline
CYP enzyme metabolism of, 158t
norepinephrine uptake and, 41
selectivity ratio of, 41
serotonin uptake and, 41
Obsessive-compulsive disorder
fluvoxamine for, 18
SSRIs for, 91
Omeprazole, 159t
Opiate(s), 158t
Oral contraceptive(s), drug interactions with, 152t
Oxidative metabolism, 137,
139
Paclitaxel, 159t
Pain, chronic, depression prevalence with, 162t
Panic disorder, SSRIs for, 91
Paracetamol, 158t
Parkinson's disease
CYP enzyme 2D6 and, 138-140
depression prevalence with, 162t
Paroxetine
brand names of, by country, 234t-236t
clearance of, age and gender and, 121t,
124-125
CYP enzymes and
2C9/10 and, 193t
2C19 and, 193t
2D6 and, 179t,
185, 186-187,
228t
2D6 deficiency and, 163,
165t
3A3/4 and, 193t
inhibition by, 170t-171t
metabolism of, 158t
development of, 16
dopamine uptake and, 39t
dosage of
age and, plasma level
and, 121t
efficacy and, 85
potency and, 50t,
51-52
drug interactions with, 152t-153t,
189, 190
effects of, on specific CYP enzymes, 176t-177t
efficacy of, acute, 92t,
93-95
half-life of, 60t,
109t, 118t,
119, 122
cirrhosis and, 127t
metabolism of, 111t,
113-114
metabolites of, 116
norepinephrine uptake and, 38t,
41
pharmacokinetics of, 109t
linear versus nonlinear,
117-119
renal disease and, 126,
127t
relapse rate with, 92t,
98-99
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
dosage and, 50t,
51-52
side effects of
discontinuation rate from,
84
incidence of, 82t-83t,
86t
steady-state of, time to, 123
structural formula of, 17
in vitro profile of, 53
washout of, 123
withdrawal from, 122-123
Perhexiline, 158t
Perphenazine, 158t
Pharmacokinetics, linear versus nonlinear, 117-119
Phenformin, 158t
Phenobarbital, drug interactions with, 152t
Phenothiazine(s), development of, 20
Phenylpiperazine (Nefazodone)
action mechanism of, 16t,
25t
CYP enzyme metabolism of, 158t-159t
drug interactions with, 155
Phenytoin
CYP enzyme metabolism of, 158t
drug interactions with, 152t,
156, 181,
193t
Potency, determination of, 33-35,
35
Prazosin, 25t
Priapism, 49t
Progesterone, 159t
Propafenone, 158t-159t
Propranolol
CYP enzyme metabolism of, 158t
drug interactions with, 152t
Protein binding, concentration dependence of, 108
Quinidine
action mechanism of, 25t
CYP enzyme metabolism of, 159t
drug interactions with, 152t
Renal disease
depression prevalence with, 162t
SSRI metabolism and, 125-126,
127t, 128
Respiratory disturbance, SSRIs and, 83t,
86t
Rifampin, drug interactions with, 152t
Risperidone
antipsychotic efficacy of, dosage and, 146,
147
CYP enzyme metabolism of, 148, 158t
side effects of, 147,
148
Secobarbital, drug interactions with, 152t
Seizure
bupropion and, 149,
150
clozapine and, 148,
149
sodium channel blockade and, 49t
Selective serotonin reuptake inhibitor(s) (SSRIs). See SSRI(s).
Serotonin uptake
antidepressant potency and, 37t,
40, 41
blockade of, consequences of, 48t
citalopram enantiomers and, 44t
dosage, plasma level, potency and, 50t
drug selectivity and, 42,
44t-45t
physiology of, 28-29
SSRI metabolites and, 57,
58t, 60t
Sertraline. See also Desmethylsertraline.
action mechanism of, 25t
brand names of, by country, 234t-236t
clearance of, age and gender and, 121t,
124-125
CYP enzymes and
2C9/10 and, 193t
2C19 and, 193t
2D6 and, 179t,
185, 187,
188-189, 230t
2D6 deficiency and, 165t
3A3/4 and, 193t
inhibition by, 170t-171t
metabolism of, 159t
development of, 16
dopamine uptake and, 39t
dosage of
age and, plasma level
and, 121t
potency and, 50t,
51-52, 85
drug interactions with, 181,
182-183, 188-189,
190
effects of, on specific CYP enzymes, 176t-177t
efficacy of
acute, 92t,
93-96, 97
dosage and, 50t,
51-52
half-life of, 60t,
109t, 118t,
122
cirrhosis and, 127t
metabolism of, 111t,
114-115
metabolites of, 116-117
potency of, 57,
58t
norepinephrine uptake and, 38t,
41
pharmacokinetics of, 109t,
114-115
linear versus nonlinear,
117-119
relapse rate with, 92t,
98-99
selectivity of, 41,
46t
serotonin uptake and, 37t,
41
dosage and, 50t,
51-52
side effects of, 70
discontinuation rate from,
84
incidence of, 82t-83t,
86t
steady-state of, time to, 123
structural formula of, 17
in vitro profile of, 53
washout of, 123
Sexual dysfunction
amitriptyline and, 70
norepinephrine uptake blockade and, 48t
serotonin uptake blockade and, 48t
sertraline and, 70
SSRIs and, 86t,
87, 88t-89t
Signal-to-noise ratio
in drug development, 24
enantiomeric form and, 30
Site of action
concentration dependence of, 35
definition of, 18-20,
19
Sodium channel blockade
consequences of, 49t
by tricyclic antidepressants, 54
Somnolence
amitriptyline and, 70
sertraline and, 70
Sparteine, 158t
SSRI(s). See also specific drug, eg, Fluoxetine.
action mechanism of, 28
action sites of, 23-24,
52
advantages of, 28
brand names of, by country, 234t-236t
chirality of, 29-32
clearance of
age and gender and, 120t-121t,
124-125
organ impairment and,
125-126, 127t,
128-129
concentration-dependent effects of, 107-108,
108t
active metabolites and,
115-117
age and gender and, 120t-121t,
124-125
antidepressant efficacy
as, 50t, 101-105,
103
half-life as, 109t,
118t, 122-123,
123
metabolism as, 110-115
organ impairment and,
125-126, 127t,
128-129
pharmacokinetics as, 117-119
plasma level as, 120t-121t
protein binding as, 108
cost of, 72-73
current popularity of, 13
CYP enzymes and, 98
affinity for, 56
inhibition by, 78
metabolism of, 158t
development of, 16,
18, 23-24
discontinuation of, because of side effects,
84
dosage of
age and, 120t-121t
efficacy and, 85
plasma level and potency
and, 50t, 51-52
drug interactions with, 77-80
efficacy of, 69,
71t, 72
acute, 91-98
concentration dependence
of, 50t, 101-105,
103
on dopamine uptake, 39t,
40
dose and, 85
metabolites and, 60t
on norepinephrine uptake,
38t, 40
on serotonin uptake, 37t,
40
examples of, 15
half-lives of, 60t,
109t, 118t,
122-123, 123
cirrhosis and, 126
for major depression, 75t
metabolism of, 110-115
metabolites of, 57,
59, 115-117
action mechanisms of,
60t
clinical relevance of,
61-62
half-lives of, 60t
potency of, 57,
58t, 60t
monoamine oxidase inhibitor interaction
with, 48t, 79-80,
144-145
for obsessive-compulsive disorder, 91
overdose of, 77-78
for panic disorder, 91
pharmacokinetics of, linear versus
nonlinear, 117-119
physician comfort level with, 63
plasma level of, dose and age and, 120t-121t
for premature ejaculation, 91
protein binding of, 108
safety of, 64-67,
65t, 77-80
selectivity of, 28-29,
46t
biogenic amine uptake
and, 42, 44t-46t,
48t-49t
and effects on different
neuroreceptors, 52, 53,
54-56
side effects of, 65t,
67-69, 70
determination of, 80
discontinuation rate from,
84
dose dependence of, 81,
87, 88t,
98
incidence of, 81,
82t-83t, 86t
sexual, 87,
88t-89t
similarities in, 75-105
steady-state of, time to, 123
switching among, 98
therapeutic monitoring of, 73-74,
99-105
versus tricyclic antidepressants,
differences in, 63-74
washout of, 80,
123
withdrawal from, 122-123
Steroid(s), 159t
Stroke, depression prevalence with, 162t
Sweating
imipramine and, 68t
SSRIs and, 83t,
86t
Sympathomimetic amine(s), antidepressant interaction with,
48t
Tachycardia
acetylcholine receptor blockade and, 48t
norepinephrine uptake blockade and, 48t
Tacrolimus, 159t
Tamoxifen, 159t
Terfenadine
cardiac arrhythmias and, 155
CYP enzyme metabolism of, 151,
155, 159t
drug interactions with, 153t,
155, 190-191
Testosterone, 159t
Theophylline
CYP enzyme metabolism of, 158t
drug interactions with, 152t
Therapeutic drug monitoring
to adjust dose upward, 101
to avoid toxicity, 100-101
decision making and, 104-105
of enantiomer, 30
fixed-dose studies as, 102
lack of incentive for, 102
of SSRIs, 73-74,
99-105
of tricyclic antidepressants, 26,
73-74
Thioridazine, 158t
Timolol, 158t
Tolbutamide
CYP enzyme metabolism of, 158t
drug interactions with, 181,
193t
Trazodone, 158t
Tremor
amitriptyline and, 70
imipramine and, 68t
norepinephrine uptake blockade and, 48t
sertraline and, 70
SSRIs and, 82t,
86t
Triacetyloleandomycin, 159t
Triazolam, 159t
Tricyclic antidepressant(s). See also specific drug, eg, Amitriptyline.
action mechanisms of, 16t,
22, 23-25,
150-151
alcohol interaction with, 65-66
antihistamine effects of, 65
antihypertensive drug interaction with,
48t-49t, 66-67
cardiac effects of, 55,
67, 74
clearance of, 24-25,
54-55, 151
cost of, 72-73
CYP enzyme metabolism of, 151,
158t
demethylation of, 55
potency and, 56
development of, 20t,
20-21
drug interactions with, 152t,
178-179, 184
evolution of, 22
for major depression, 72
monitoring intake of, 26
overdose of, 24,
65, 77
CYP enzyme 2D6 deficiency
and, 100-101
symptoms of, 26,
151
pharmacokinetics of, 151
potency of, 69,
71t, 72
dopamine uptake and, 39t,
40
norepinephrine uptake
and, 38t, 40
serotonin uptake and,
37t
response curves of, multiple concentrations
and, 154
safety of, 64-67,
65t
selectivity of, 46t
biogenic amine uptake
and, 42, 44t-46t,
48t-49t
side effects of, 25-26,
65t, 67-69,
68t, 70
clearance rate and, 54-55
sodium channel blockade by, 54
versus SSRIs, 63-74
therapeutic monitoring of, 73-74
Trimipramine, 158t
Tryptophan, SSRI interaction with, 48t
Tumor, terminal solid, depression prevalence with, 162t
Urinary frequency
imipramine and, 68t
SSRIs and, 83t,
86t
Urinary retention
acetylcholine receptor blockade and, 48t
imipramine and, 68t
SSRIs and, 83t
Valproate, drug interactions with, 156
Venlafaxine
action mechanism of, 16t
CYP enzyme metabolism of, 158t
Verapamil, 159t
Visual disturbance
acetylcholine receptor blockade and, 48t
amitriptyline and, 70
imipramine and, 68t
sertraline and, 70
SSRIs and, 82t
Vomiting, serotonin uptake blockade and, 48t
Warfarin
CYP enzyme metabolism of, 158t,
180-181
drug interactions with, 152t,
180-181
Weight gain, histamine receptor blockade and, 48t
Withdrawal syndrome, 122-123
Yohimbine, action mechanism of, 25t
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