Table 2.
Drugs used to treat psychiatric and neurological conditions that target serotonin receptors and their side effects in women and men. Data obtained from EMA and FDA drug approving bodies, SIDER and DrugBank. Abbreviations: MDD, multiple personality disorder; OCD, obsessive compulsive disorder; GAD, generalized anxiety disorder; PMDD, premenstrual dysphoric disorder; SAD, social anxiety disorder; PD, panic disorder; 5-HT, serotonin. Orange coloured cells represent excitatory receptors and blue represents inhibitory receptors.
| Generic Drug Name | Treatment | Side effect seen more in women than in men | Side effect seen more in men than in women | 5-HT receptor Target | Antagonist/Agonist | References |
|---|---|---|---|---|---|---|
| Cisapride | Anti-heart burn | Fatal heart disturbance, vaginitis, reproductive failure, galactorrhoea | Gynecomastia | 5-HT2a | Agonist | (49, 50) |
| 5-HT2c | ||||||
| 5-HT4 | ||||||
| Cyproheptadine Hydrochloride | Hypersensitivity Reactions symptoms | None reported | None reported | 5-HT2a | Antagonist | (49–51) |
| 5-HT2b | ||||||
| 5-HT2c | ||||||
| 5-HT7 | ||||||
| Fenfluramine Hydrochloride | Dravet Syndrome | None reported | None reported | 5-HT1a | Agonist | (50, 52) |
| 5-HT1d | ||||||
| 5-HT2a | ||||||
| 5-HT2b | ||||||
| 5-HT2c | ||||||
| Amisulpride | Schizophrenia, PONV | Vaginal inflammation, menstrual disorder, pregnancy risk increase, infertility | Ejaculatory dysfunction | 5-HT2a | Antagonist | (50, 52–54) |
| 5-HT2b | ||||||
| 5-HT7 | ||||||
| Aripiprazole Mylan | Schizophrenia, Bipolar I | Decreased libido, tardive dyskinesia (older women), weight gain | Erectile dysfunction, dystonia | 5-HT1a | Partial agonist | (49, 50, 52, 55) |
| 5-HT1b | Antagonist | |||||
| 5-HT1d | ||||||
| 5-HT2a | ||||||
| 5-HT2c | Antagonist, partial agonist | |||||
| 5-HT7 | ||||||
| Cariprazine Hydrochloride | Schizophrenia, Bipolar | Tardive dyskinesia (older women), decrease fertility, amenorrhea, vaginitis | Ejaculation dysfunction | 5-HT1a | Partial agonist | (18, 49, 50) |
| 5-HT2a | Antagonist | |||||
| 5-HT2b | ||||||
| Clozapine | Schizophrenia, Suicidal | Tardive dyskinesia, agranulocytosis (older women), breast cancer, weight gain | Acute dystonia, abnormal ejaculation | 5-HT1a | Antagonist | (49–51, 53) |
| 5-HT1b | ||||||
| 5-HT1d | ||||||
| 5-HT1e | ||||||
| 5-HT2a | ||||||
| 5-HT2c | ||||||
| 5-HT6 | ||||||
| 5-HT7 | ||||||
| Fanaptum | Schizophrenia | Breast discharge, abnormal menstrual cycle, fertility decrease | Ejaculation failure | 5-HT1a | Antagonist | (50, 52) |
| 5-H2a | ||||||
| 5-HT6 | ||||||
| Flupentixol | Schizophrenia, Antidepressant | Amenorrhea, decreased fertility, hyperprolactinemia, galactorrhoea, decrease libido | Erectile dysfunction, ejaculation failure | 5-HT2a | Antagonist | (50) |
| 5-HT2C | ||||||
| Iloperidone | Schizophrenia | Galactorrhoea, menstruation irregular, menorrhagia, metrorrhagia, postmenopausal haemorrhage | Gynecomastia, erectile dysfunction, prostatitis | 5-HT1a | Antagonist | (50, 56) |
| 5-HT2a | ||||||
| 5-HT6 | ||||||
| 5-HT7 | ||||||
| Lumateperone Tosylate | Schizophrenia, Bipolar, Depression | Tardive dyskinesia (older women) | Acute dystonia | 5-HT2a | Antagonist | (49, 50) |
| 5-HT2c | ||||||
| Lurasidone | Bipolar 1, Schizophrenia | Amenorrhea, decreased lactation | Erectile dysfunction | 5-HT1a | Antagonist | (50, 53, 57) |
| 5-HT1c | ||||||
| 5-HT2a | ||||||
| 5-HT7 | ||||||
| Olanzapine | Bipolar, Schizophrenia | Menstrual disorder, vaginal inflammation, vaginal discharge, menorrhagia, metrorrhagia, premenstrual syndrome, female lactation, uterine fibroids enlarged, vaginal haemorrhage, amblyopia, vaginitis | Erectile dysfunction | 5-HT2a | Antagonist | (50) |
| 5-HT2c | ||||||
| 5-HT6 | ||||||
| Paliperidone | Schizophrenia | Amenorrhea, decreased lactation, pregnancy risk increase | Erectile dysfunction | 5-HT1a | Antagonist | (50, 51) |
| 5-HT1d | ||||||
| 5-HT2a | ||||||
| 5-HT2c | ||||||
| 5-HT1a | ||||||
| Quetiapine | Bipolar | Vaginal inflammation, female lactation, vaginal infection increase, vulvovaginitis, vaginal moniliasis, vaginitis, metrorrhagia, cystitis, amenorrhea, lactation, leukorrhea, vaginal haemorrhage, vulvovaginitis orchitis | Erectile dysfunction, abnormal ejaculation, gynecomastia | 5-HT1a | Antagonist, partial agonist | (50, 53) |
| 5-HT2a | Antagonist | |||||
| 5-HT6 | ||||||
| Risperdal Consta | Schizophrenia, Bipolar Disorder | Tardive dyskinesia (elder women), thrombotic thrombocytopenic purpura, pituitary gland adenomas, impaired fertility, menstrual disorder, breast cancer, disorder and pain and vaginal inflammation, dryness and haemorrhage, unintended pregnancy, menstruation delayed, menstrual disorder, amenorrhea | Acute dystonia, erectile dysfunction, gynecomastia | 5-HT1a | Antagonist | (49–51) |
| 5-HT1c | ||||||
| 5-HT1d | ||||||
| 5-HT2a | ||||||
| 5-HT7 | ||||||
| Ziprasidone | Bipolar, Schizophrenia | Menorrhagia, metrorrhagia, female lactation, uterine and vaginal haemorrhage, sexual dysfunction, uterine haemorrhage, menorrhagia, female lactation, amenorrhea, metrorrhagia | Erectile dysfunction, abnormal ejaculation, male sexual dysfunction | 5-HT1a | Agonist | (50, 51) |
| 5-HT1b | ||||||
| 5-HT1d | ||||||
| 5-HT1e | ||||||
| 5-HT2a | ||||||
| 5-HT2c | ||||||
| 5-HT6 | ||||||
| 5-HT5a | ||||||
| 5-HT7 | ||||||
| Citalopram | Anti-depressant | Breast pain, enlargement and discharge, endocrine disorder, amenorrhea, galactorrhoea, menstrual disorder, vaginal discharge, infection increase, dryness, inflammation, haemorrhage, pain and discharge, unintended pregnancy | Testicular disorder, testicular pain, ejaculation disorder | 5-HT2a | Antagonist | (51, 52) |
| Imipramine Pamoate | Anti- Depressant | Breast enlargement, galactorrhoea | Gynecomastia, ineffectiveness, testicular swelling | 5-HT1a | Agonist | (49–51) |
| 5-HT2a | Antagonist | |||||
| 5-HT2c | ||||||
| 5-HT7 | ||||||
| 5-HT6 | Partial agonist | |||||
| Nefazodone Hydrochloride | Anti-Depressant | Vaginitis, breast pain, uterine haemorrhage, uterine fibroids enlarged, menorrhagia | Galactorrhoea, erectile dysfunction, gynecomastia | 5-HT1a | Antagonist | (49–51) |
| 5-HT2a | ||||||
| 5-HT2c | ||||||
| Clomipramine | OCD, MDD | Menstrual disorder, vaginal and uterine inflammation, ovarian cysts, uterine and vaginal haemorrhage, endometrial hyperplasia, uterine inflammation, amenorrhea, breast pain, breast enlargement, leukorrhea, vaginitis, dysmenorrhea | Erectile dysfunction, prostatic disorder, testicular swelling, impotence | 5-HT2a | Antagonist | (52, 54, 58) |
| 5-HT2b | ||||||
| 5-HT2c | ||||||
| Escitalopram | MDD, GAD, OCD | Impair fertility, interference with fallopian tube motility, breast disorder, pain, enlargement and cancer risk, menstrual disorder, ovarian cyst, premenstrual disorder, vaginitis atrophic, vaginal discharge, infection increase, dryness, pain and haemorrhage | Ejaculation disorder, testicular pain, gynecomastia | 5-HT1a | Antagonist | (50–52) |
| 5-HT2a | ||||||
| 5-HT2c | ||||||
| Paroxetine | MDD, Panic disorder, OCD, social phobia, GAD, PMDD, vasomotor, menopausal symptoms | Abdominal pain, attention disturbance, suicidal ideation, bone fractures, agitation, impaired fertility, interference with fallopian tube motility, menstrual disorder, breast pain, ovarian cyst, vaginal infection increase and inflammation, uterine spasm, uterine sertraline enlarged, endometrial disorder | Erectile dysfunction, testicular pain, breast atrophy, endometrial disorder, gynecomastia | 5-HT2a | Agonist | (49–51) |
| 5-HT2b | ||||||
| Nortriptyline | MDD | Galactorrhoea, breast enlargement | Erectile dysfunction | 5-HT1a | Antagonist | (50) |
| 5-HT1c | ||||||
| 5-HT2a | ||||||
| 5-HT2b | ||||||
| 5-HT2c | ||||||
| Desipramine | MDD | Menstrual disorder, galactorrhoea, breast enlargement | Gynecomastia, erectile dysfunction | 5-HT1a | Partial antagonist, agonist | (49) |
| 5-HT2a | Antagonist | |||||
| 5-HT2c | Partial antagonist, agonist | |||||
| Trazodone Hydrochloride | MDD | Lactation, clitorism | Priapism | 5-HT1a | Antagonist | (49, 50) |
| 5-HT1c | ||||||
| 5-HT2a | Antagonist, partial agonist | |||||
| 5-HT2b | ||||||
| 5-HT2c | ||||||
| Trimipramine Maleate | MDD | Galactorrhoea, breast enlargement | Gynecomastia, erectile dysfunction | 5-HT1a | Antagonist | (49) |
| 5-HT2c | ||||||
| 5-HT1d | Partial agonist, antagonist | |||||
| 5-HT2a | Agonist | |||||
| Vortioxetine | MDD | Sexual dysfunction | None reported | 5-HT1a | Agonist | (50) |
| 5-HT1b | Partial agonist | |||||
| 5-HT7 | Antagonist | |||||
| Almotriptan Malate | Migraine | Dysmenorrhea | None reported | 5-HT1b | Agonist | (50, 51) |
| 5-HT1d | ||||||
| Dihydroergotamine Mesylate | Migraine | Reproductive malfunction, pelvic inflammation, vaginitis, vaginal inflammation | None reported | 5-HT1a | Agonist | (49–51) |
| 5-HT1d | ||||||
| 5-HT2a | ||||||
| 5-HT2c | ||||||
| Eletriptan Hydrobromide | Migraine | Vaginal inflammation, menstrual disorder, menorrhagia | Erectile dysfunction | 5-HT1a | Agonist | (50, 51) |
| 5-HT1b | ||||||
| 5-HT1d | ||||||
| 5-HT1f | ||||||
| Frovatriptan | Migraine | None reported | None reported | 5-HT1b | Agonist | (50) |
| 5-HT1d | ||||||
| Methysergide Maleate | Migraine | Vasoconstrictive phenomena, hair loss, ineffectiveness | Mild temporal lobe disturbance | 5-HT1a | Agonist | (49–51, 59) |
| 5-HT2a | Antagonist | |||||
| 5-HT2b | ||||||
| 5-HT2c | ||||||
| 5-HT7 | ||||||
| Naratriptan | Migraine | Vaginal inflammation, fallopian tube inflammation, endometrium disorder | None reported | 5-HT1a | Agonist | (50) |
| 5-HT1b | ||||||
| 5-HT1d | ||||||
| 5-HT1f | ||||||
| Sumatriptan | Migraine | Endometriosis, breast discharge, tenderness, lactation, cysts, lumps, abnormal menstrual cycle, breast cancer, dysmenorrhea, intermenstrual bleeding, abortion, menstruation symptoms, abnormal menstrual cycle, inflammation of fallopian tubes | None reported | 5-HT1a | Agonist | (49–51) |
| 5-HT1b | ||||||
| 5-HT1d | ||||||
| 5-HT1f | ||||||
| 5-HT5a | ||||||
| 5-HT7 | ||||||
| Zolmitriptan | Migraine | Vaginal inflammation, uterine disorder, uterine fibroids enlarged | None reported | 5-HT1a | Agonist | (50, 51) |
| 5-HT1b | ||||||
| 5-HT1d | ||||||
| 5-HT1e | ||||||
| 5-HT1f | ||||||
| 5-HT2a | ||||||
| 5-HT2b | ||||||
| 5-HT7 |