amitriptyline

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A tricyclic antidepressant drug, C₂₀H₂₃N.

[Perhaps AMI(NO)– + alteration of TRYPT(OPHAN) + –YL + –INE².]

Definition

Amitriptyline is a medication used to treat various forms of depression, pain associated with the nerves (neuropathic pain), and to prevent migraine headaches. It is sold in the United States under the brand name Elavil.

Purpose

Amitriptyline helps relieve depression and pain. It is often used to manage nerve pain resulting from cancer treatment. Such injury to nerves causes a burning, tingling sensation. This medication, usually given at bedtime, helps patients sleep better.

Description

This medication is one of several tricyclic antidepressants. Amitriptyline acts to block reabsorption of chemicals that transmit nerve messages in the brain.

Recommended Dosage

Amitriptyline's usual adult dose for pain management is 10 mg to 150 mg at bedtime. Patients are generally started on a low dose. The amount of medication may be increased as needed. Side effects, such as a dry mouth and drowsiness, may make it difficult to increase the dose in older adults. Bedtime dosing helps the patient sleep. Doctors generally order 75 mg to 150 mg for depression. It is given at bedtime or in divided doses. It may take 30 days for the patient to feel less depressed. Pain relief is usually noticed sooner than the mood change. Teens and older adults usually receive a lower dose. If the nightly dose is missed, it should not be taken the next morning. Taking amitriptyline during waking hours could result in noticeable side effects. Patients should check with their doctor if the daily dose is missed. Those on more than one dose per day should take a missed dose as soon as it is noted. Patients should not take two doses at the same time. Injectable amitriptyline is available. It should not be used long-term. Patients should switch to tablets as soon as possible.

Precautions

Patients should not suddenly stop taking this medication. The dose should gradually be decreased, then discontinued. If the drug is abruptly stopped, the patient may experience headache, nausea, discomfort throughout the body, and a worsening of original symptoms. Amitriptyline's effects last for three to seven days after the medication has been stopped. Older adults usually are more prone to some side effects. These include drowsiness, dizziness, mental confusion, blurry vision, dry mouth, difficulty urinating, and constipation. Taking a lower dose may help resolve these problems. Patients may need to stop this medication before surgery.

Amitriptyline should not be given to anyone with allergies to the drug or to patients recovering from a heart attack. Patients taking MAO inhibitors, a different type of antidepressant, should not also use amitriptyline. It should be administered with caution to patients with glaucoma, seizures, urinary retention, an overactive thyroid, poor liver or kidney function, alcoholism, asthma, digestive disorders, an enlarged prostate, seizures, or heart disease. This medication should not be given to children under 12. Pregnant women should discuss the risks and benefits of this medication with their doctor. Fetal deformities have been associated with taking this drug during pregnancy. Women should not breastfeed while using amitriptyline.

Side Effects

Common side effects associated with amitriptyline include dry mouth, drowsiness, constipation, and dizziness or lightheadedness when standing. Patients can suck on ice cubes or sugarless hard candy to combat the dry mouth. Increased fiber in the diet and additional fluids may help the constipation. The dizziness is usually caused by a drop in blood pressure when changing position. Patients should slowly rise from a sitting or lying position if dizziness is noticed. Amitriptyline may increase the risk of falls in older adults. Patients should not drive or operate machinery or appliances while under the influence of this drug. Alcohol and other central nervous system depressants can increase drowsiness. Amitriptyline may also produce blurry vision and an irregular or fast heartbeat. Amitriptyline also may raise or lower blood pressure, or cause palpitations. This medication may increase or decrease diabetic patients' blood sugar levels. Amitriptyline may make patients' skin more sensitive to the sun. Patients should avoid direct sunlight, wear protective clothing, and apply sunscreen with a protective factor of 15 or higher.

Amitriptyline may increase appetite, cause weight gain, or produce an unpleasant taste in the mouth. It may also cause diarrhea, vomiting, or heartburn. Taking this medication with food may decrease digestive side effects. Other less likely side effects include muscle tremors, nervousness, impaired sexual function, sweating, rash, itching, hair loss, ringing in the ears, or changes in the make up of the patient's blood. Patients with schizophrenia may develop an increase in psychiatric symptoms.

Interactions

Patients should always tell all doctors and dentists that they are taking this medication. Amitriptyline may decrease the effectiveness of some drugs used to treat high blood pressure. Amitriptyline should not be taken with other antidepressants, epinephrine and other adrena-line-type drugs, or methylphenidate. Patients should not take over-the-counter medications without checking with their doctor. For instance, amitriptyline should not be taken with Tagamet (cimetidine) or Neo-Synephrine. Patients taking this drug should avoid the dietary supplements St. John's wort, belladonna, henbane and scopolia. Black tea may decrease the absorption of this drug. Patients should ingest the drug and tea at least two hours apart.

—Debra Wood, R.N.

Brand names: Elavil®, Tryptanol™, Vanatrip®

Chemical formula:

Drug Forms:
• Amitriptyline Hydrochloride Oral tablet (below)
• Amitriptyline tablets
• Amitriptyline injection

Español:
• Amitriptilina Clorhidrato, Tableta oral
• Tabletas de amitriptilina
• Inyección de amitriptilina

Amitriptyline Hydrochloride Oral tablet

What is this medicine?

AMITRIPTYLINE is used to treat depression.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• an alcohol problem
• asthma, difficulty breathing
• bipolar disorder or schizophrenia
• difficulty passing urine, prostate trouble
• glaucoma
• heart disease or previous heart attack
• liver disease
• over active thyroid
• seizures
• thoughts or plans of suicide, a previous suicide attempt, or family history of suicide attempt
• an unusual or allergic reaction to amitriptyline, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Take this medicine by mouth with a drink of water. Follow the directions on the prescription label. You can take the tablets with or without food. Take your medicine at regular intervals. Do not take it more often than directed. If you have been taking this medicine regularly for some time, do not suddenly stop taking it. You must gradually reduce the dose or you may get severe side effects. Ask your doctor or health care professional for advice. Even after you stop taking this medicine it can still affect your body for several days.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
• arsenic trioxide
• certain medicines used to regulate abnormal heartbeat or to treat other heart conditions
• cisapride
• droperidol
• halofantrine
• MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate
• other medicines for mental depression
• phenothiazines like perphenazine, thioridazine and chlorpromazine
• pimozide
• probucol
• procarbazine
• sparfloxacin
• St. John's Wort
• ziprasidone

This medicine may also interact with the following medications:
• atropine and related drugs like hyoscyamine, scopolamine, tolterodine and others
• barbiturate medicines for inducing sleep or treating seizures, like phenobarbital
• cimetidine
• disulfiram
• ethchlorvynol
• thyroid hormones such as levothyroxine

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. It can take several days before you feel the full effect of this medicine.

Patients and their families should watch out for worsening depression or thoughts of suicide. Also watch out for sudden or severe changes in feelings such as feeling anxious, agitated, panicky, irritable, hostile, aggressive, impulsive, severely restless, overly excited and hyperactive, or not being able to sleep. If this happens, especially at the beginning of antidepressant treatment or after a change in dose, call your health care professional.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may increase dizziness and drowsiness. Avoid alcoholic drinks.

Do not treat yourself for coughs, colds, or allergies without asking your doctor or health care professional for advice. Some ingredients can increase possible side effects.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water will help.

This medicine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your eye doctor if the problem does not go away or is severe.

This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.

If you are diabetic, check your blood sugar more often than usual, especially during the first few weeks of treatment with this medicine. This medicine can affect blood sugar levels. Call your doctor or health care professional for advice if you notice a change in the results of blood or urine glucose tests.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• abnormal production of milk in females
• breast enlargement in both males and females
• breathing problems
• confusion, hallucinations
• fast, irregular heartbeat
• fever with increased sweating
• muscle stiffness, or spasms
• pain or difficulty passing urine, loss of bladder control
• seizures
• suicidal thoughts or other mood changes
• swelling of the testicles
• tingling, pain, or numbness in the feet or hands
• yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• change in sex drive or performance
• constipation or diarrhea
• nausea, vomiting
• weight gain or loss

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A tricyclic antidepressant in humans; used in dogs and cats to treat psychodermatosis and as an antipruritic.

Amitriptyline
Systematic (IUPAC) name
3-(10,11-dihydro-5H-dibenzo[[a,d]] cycloheptene-5-ylidene)-N, N-dimethyl-1-propanamine
Identifiers
CAS number	50-48-6
ATC code	N06AA09
PubChem	2160
DrugBank	APRD00227
ChemSpider	2075
Chemical data
Formula	C20H23N
Mol. mass	277.403 g/mol
Pharmacokinetic data
Bioavailability	40%
Metabolism	Hepatic
Half life	12–24 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	D(US)
Legal status	Unscheduled(AU) POM(UK)
Routes	Oral

Amitriptyline (or Amitryptyline) hydrochloride (sold as Elavil, Tryptanol, Endep, Elatrol, Tryptizol, Trepiline, Laroxyl, Saroten, Triptyl, Redomex) is a tricyclic antidepressant drug. It is a white, odorless, crystalline compound which is freely soluble in water; it is usually dispensed in tablet form. In terms of its mechanism of action, amitriptyline inhibits serotonin^[1] and noradrenaline reuptake almost equally.

Contents 1 Uses 1.1 Approved 1.2 Unapproved/off-label/investigational use 2 Side effects 3 Overdose 4 Footnotes 5 References

Uses

Amitriptyline is now used in the United States and UK to prevent migraines only in very small doses. It is also used as sleeping aids in small doses of usually 25 mg.

Approved

Amitriptyline is approved most commonly for the treatment of major depression. (clinical/endogenous depression, also Involutional melancholia 'depression of late life', which is no longer seen as a disease in its own right). Adult typical dosages are 25 to 150 mg daily, with half this initially for elderly or adolescents.

Children between the ages of 7 to 10 years having a dose of 10 to 20 mg, older children 25 to 50 mg at night. It should be gradually withdrawn at the end of the course, which overall should be of no more than 3 months.^[2]

Amitriptyline is used in ankylosing spondylitis for pain relief and in some European countries it is officially approved as a preventive (for patients with frequent/chronic migraines, usually 25 to 75 mg.

Unapproved/off-label/investigational use

Amitriptyline may be prescribed for other conditions such as insomnia, PTSD^[3], migraine, rebound headache, chronic pain, tinnitus, chronic cough, postherpetic neuralgia (persistent pain following a shingles attack), carpal tunnel syndrome, fibromyalgia, vulvodynia, interstitial cystitis, male chronic pelvic pain syndrome, irritable bowel syndrome, diabetic peripheral neuropathy, neurological pain, and painful paresthesias related to multiple sclerosis and at low doses as a preventive (prophylaxis) for patients with frequent migraines.^[4] Typically lower dosages are required for pain modification of 10 to 50 mg daily.^[2]

Amitriptyline in low doses is also sometimes prescribed to help ease the symptoms of chronic fatigue syndrome. It is thought to help combat symptoms of insomnia primarily, in addition to other selected symptoms of the affliction.

A randomized controlled trial published in June 2005 found that amitriptyline was effective in functional dyspepsia that did not respond to a first-line treatment (famotidine or mosapride).^[5]

Side effects

Common side effects of using amitriptyline are mostly due to its anticholinergic activity, including: weight gain, dry mouth, loss of appetite, drowsiness, muscle stiffness, nausea, constipation, nervousness, dizziness, blurred vision, urinary retention and insomnia. Some rare side effects include tinnitus, hypotension, mania, psychosis, heart block, arrhythmias, lip and mouth ulcers, extrapyramidal symptoms, depression, and hepatic toxicity.

Overdose

Main article: Tricyclic antidepressant overdose

The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants.

Footnotes

1. ^ Bendtsen L, Jensen R, Olesen J (September 1996). "A non-selective (amitriptyline), but not a selective (citalopram), serotonin reuptake inhibitor is effective in the prophylactic treatment of chronic tension-type headache". Journal of neurology, neurosurgery, and psychiatry 61 (3): 285–90. doi:10.1136/jnnp.61.3.285. PMID 8795600. 
2. ^ ^{a b} British National Formulary 45 (March 2003).
3. ^ National Institute for Clinical Excellence: The Treatment of PTSD in Adults and Children
4. ^ Ziegler D, Hurwitz A, Hassanein R, Kodanaz H, Preskorn S, Mason J (1987). "Migraine prophylaxis. A comparison of propranolol and amitriptyline". Arch Neurol 44 (5): 486–9. PMID 3579659. 
5. ^ Otaka M, Jin M, Odashima M, et al. (June 2005). "New strategy of therapy for functional dyspepsia using famotidine, mosapride and amitriptyline". Aliment. Pharmacol. Ther. 21 (Suppl 2): 42–6. doi:10.1111/j.1365-2036.2005.02473.x. PMID 15943846. http://www.ingentaconnect.com/content/bsc/apt/2005/00000021/A00201s2/art00008. 

References

• PubChem Substance Summary: Amitriptyline National Center for Biotechnology Information.
• TREPILINE-10 TABLETS; TREPILINE-25 TABLETS South African Electronic Package Inserts. 12 May 1978. Revised February 2004.
• SAROTEN RETARD 25 mg Capsules; SAROTEN RETARD 50 mg Capsules South African Electronic Package Inserts. December 1987. Updated May 2000.
• AMITRIP Amitriptyline hydrochloride 10 mg, 25 mg and 50 mg Capsules Medsafe NZ Physician Data Sheet. November 2004.
• Endep Consumer Medicine Information, Australia. December 2005.
• MedlinePlus Drug Information: Amitriptyline. US National Institutes of Health. January 2008.

v • d • e Antidepressants SSRIs Citalopram • Dapoxetine • Escitalopram • Femoxetine • Fluoxetine • Fluvoxamine • Paroxetine • Sertraline • Vilazodone • Zimelidine SNRIs Bicifadine • Desvenlafaxine • Duloxetine • Milnacipran • Sibutramine • Tramadol • Venlafaxine NRIs Atomoxetine • Mazindol • Nisoxetine • Reboxetine • Viloxazine NDRIs Amineptine • Bupropion • Methylphenidate • Nomifensine • Radafaxine DRIs Medifoxamine • Vanoxerine SNDRIs Brasofensine • Diclofensine • DOV 102,677 • DOV 21,947 • DOV 216,303 • NS2359 • SEP-225289 • SEP-227162 • Tesofensine SSREs Tianeptine NDRAs Amphetamine • Lisdexamfetamine • Methamphetamine • Phenethylamine TCAs Amitriptyline • Butriptyline • Cianopramine • Clomipramine • Desipramine • Dibenzepin • Dosulepin • Doxepin • Imipramine • Iprindole • Lofepramine • Melitracen • Nitroxazepine • Nortriptyline • Opipramol • Protriptyline • Trimipramine TeCAs Amoxapine • Maprotiline • Mianserin • Mirtazapine • Oxaprotiline • Setiptiline MAOIs Nonselective: Iproclozide • Iproniazid • Isocarboxazid • Nialamide • Phenelzine • Pheniprazine • Tranylcypromine MAO-A Selective: Befloxatone • Brofaromine • Cimoxatone • Clorgiline • Harmala Alkaloids • Minaprine • Moclobemide • Pirlindole • Toloxatone • Tyrima MAO-B Selective: Lazabemide • Pargyline • Rasagiline • Selegiline Direct Receptor Ligands 5-HT1A Receptor Agonists: Buspirone • Flesinoxan • Flibanserin • Gepirone • PRX-00023 • Tandospirone 5-HT2 Receptor Antagonists: Agomelatine • Etoperidone • Nefazodone • Trazodone D2-like Autoreceptor Antagonists: Amisulpride • Sulpiride D2-like Receptor Agonists: Piribedil • Pramipexole • Ropinirole • Rotigotine NMDA Receptor Antagonists: Ketamine Dietary Supplements Amino Acids: 5-HTP • L-DOPA • L-Glutamine • L-Phenylalanine • L-Tryptophan • L-Tyrosine Vitamins/Minerals: Ascorbic Acid (Vitamin C) • B-Vitamins (Folic Acid, Niacin, Pyridoxal Phosphate, etc) • Magnesium • Zinc Herbs: Curcuma Longa (Turmeric) • Eleutherococcus Senticosus (Siberian Ginseng) • Ginkgo Biloba (Ginkgo) • Glycyrrhiza Glabra (Licorice) • Hydrocotyle Asiatica (Gotu Kola) • Hypericum Perforatum (St John's Wort) • Panax Ginseng (Ginseng) • Passiflora Incarnata (Passion Flower) • Piper Methysticum (Kava Kava) • Peganum Harmala (Syrian Rue) • Rhodiola Rosea (Golden Root) • Rosmarinus Officinalis (Rosemary) • Sceletium Tortuosum (Kanna) • Schisandra Chinensis (Magnolia Vine) • Scutellaria Lateriflora (Skullcap) • Valeriana Officinalis (Valerian) • Zingiber Officinale (Ginger) Others: Inositol • Omega-3 Fatty Acids • S-Adenosyl-L-Methionine (SAMe)

v • d • e Serotonergics Receptor Ligands 5-HT1 5-HT1A Agonists: Azapirones: Alnespirone • Binospirone • Buspirone • Gepirone • Ipsapirone • Perospirone • Tandospirone • Tiospirone • Zalospirone; Lysergamides: Dihydroergotamine • Ergotamine • Methysergide • LSD; Phenethylamines: MDA • MDMA; Piperazines: Eltoprazine • Flesinoxan • Flibanserin; Tryptamines: 5-CT • 5-MeO-DMT • 5-MT • DMT • Psilocin • Psilocybin • Rauwolscine • Yohimbine; Atypical Antipsychotics: Aripiprazole • Asenapine • Clozapine • Quetiapine • Ziprasidone; Others: 8-OH-DPAT • F 11440 • F 13640 • Lesopitron • Lu AA21004 • LY293284 • LY301317 • MKC-242 • Osemozotan • Piclozotan • PRX-00023 • Repinotan • RU-24969 • S-15535 • Sarizotan • SSR-181,507 • Sunepitron • U-92016A • Urapidil • Vilazodone • Xaliproden Antagonists: Beta Blockers: Alprenolol • Cyanopindolol • Iodocyanopindolol • Oxprenolol • Pindobind • Pindolol • Propranolol; Piperazines: Nefazodone • Trazodone • WAY-100,135 • WAY-100,635; Others: AV965 • BMY-7378 • Dotarizine • GR-46611 • Isamoltane • Lecozotan • Methiothepin • MPPF • NAN-190 • Robalzotan • S-15535 • SB-649915 • SDZ 216-525 • Spiperone • Spiroxatrine • UH-301 • Xylamidine 5-HT1B Agonists: Lysergamides: Dihydroergotamine • Ergotamine • Methysergide; Piperazines: Eltoprazine • TFMPP; Triptans: Eletriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; Others: CP-93,129 • CP-94,253 • CP-135,807 • RU-24969 Antagonists: Lysergamides: Metergoline • Methiothepin; Tryptamines: Yohimbine; Others: AR-A000002 • GR-127,935 • Isamoltane • SB-216,641 • SB-224,289 • SB-236,057 5-HT1D Agonists: Lysergamides: Dihydroergotamine • Methysergide; Triptans: Almotriptan • Eletriptan • Frovatriptan • Naratriptan • Rizatriptan • Sumatriptan • Zolmitriptan; Tryptamines: 5-CT • 5-MT; Others: CP-135,807 • CP-286,601 • GR-46611 • L-694,247 • L-772,405 • PNU-109,291 • PNU-142,633 Antagonists: Lysergamides: Metergoline • Methiothepin; Tryptamines: Yohimbine; Others: BRL-15572 • GR-127,935 • Ketanserin • LY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Rauwolscine • Ritanserin • Ziprasidone 5-HT1E Agonists: Lysergamides: Methysergide; Triptans: Eletriptan; Tryptamines: Tryptamine Antagonists: Methiothepin 5-HT1F Agonists: Triptans: Eletriptan • Naratriptan • Sumatriptan; Tryptamines: 5-MT; Others: LY-334,370 Antagonists: Methiothepin 5-HT2 5-HT2A Agonists: Lysergamides: ALD-52 • Ergonovine • Lisuride • LA-SS-Az • LSD • Lysergic acid 2-butyl amide • Methysergide; Phenethylamines: 25I-NBMD • 25I-NBOH • 25I-NBOMe • 2C-B • 2C-B-FLY • 2C-E • 2C-I • 2C-T-2 • 2C-T-7 • 2C-T-21 • 2CBCB-NBOMe • 2CBFly-NBOMe • Bromo-DragonFLY • DOB • DOC • DOI • DOM • DOTFM • MDA • MDMA • Mescaline • Myristicin • TCB-2 • TFMFly; Piperazines: BZP • Quipazine • TFMPP; Tryptamines: 5-CT • 5-MeO-α-ET • 5-MeO-α-MT • 5-MeO-DET • 5-MeO-DiPT • 5-MeO-DMT • 5-MeO-DPT • 5-MT • α-ET • α-Methyl-5-HT • α-MT • Bufotenin • DET • DiPT • DMT • DPT • Psilocin • Psilocybin; Others: AL-34662 • AL-37350A • PNU-22394 Antagonists: Atypical Antipsychotics: Amperozide • Aripiprazole • Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine; Typical Antipsychotics: Loxapine • Pipamperone; Antidepressants: Amitriptyline • Amoxapine • Etoperidone • Mianserin • Mirtazapine • Nefazodone • Trazodone; Others: 5-I-R91150 • AC-90179 • Altanserin • AMDA • APD-215 • Blonanserin • Cinanserin • Cyproheptadine • Deramciclane • Dotarizine • Eplivanserin • Fananserin • Flibanserin • Ketanserin • Lubazodone • MDL-100,907 • Methiothepin • Nantenine • Pimavanserin • Pizotifen • Ritanserin • Sarpogrelate • Setoperone • SR-46349B • Xylamidine • Yohimbine 5-HT2B Agonists: Oxazolines: 4-Methylaminorex • Aminorex; Phenethylamines: Chlorphentermine • Fenfluramine • MDA • MDMA • Norfenfluramine; Tryptamines: 5-CT • 5-MT • α-Methyl-5-HT; Others: BW-723C86 • Cabergoline • mCPP • Pergolide • PNU-22394 • Ro60-0175 Antagonists: Agomelatine • Asenapine • EGIS-7625 • Ketanserin • Lisuride • LY-272,015 • Rauwolscine • Ritanserin • RS-127,445 • Sarpogrelate • SB-200,646 • SB-204,741 • SB-206,553 • SB-215,505 • SB-221,284 • SB-228,357 • SDZ SER-082 • Tegaserod • Yohimbine 5-HT2C Agonists: Piperazines: Aripiprazole • mCPP • TFMPP; Tryptamines: 5-CT • 5-MT • α-Methyl-5-HT; Others: A-372,159 • AL-38022A • CP-809,101 • Lorcaserin • MK-212 • PNU-22394 • Ro60-0175 • Vabicaserin • WAY-629 • WAY-161,503 • YM-348 Antagonists: Atypical Antipsychotics: Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Pimozide • Quetiapine • Risperidone • Sertindole • Ziprasidone • Zotepine; Typical Antipsychotics: Loxapine • Pipamperone; Antidepressants: Agomelatine • Amitriptyline • Amoxapine • Etoperidone • Fluoxetine • Mianserin • Mirtazapine • Nefazodone • Trazodone; Others: Cinanserin • Deramciclane • Dimebolin • Dotarizine • Eltoprazine • FR-260,010 • Ketanserin • Pizotifen • Ritanserin • RS-102,221 • SB-200,646 • SB-206,553 • SB-221,284 • SB-228,357 • SB-242,084 • SB-243,213 • SDZ SER-082 • Xylamidine 5-HT3 Agonists: Piperazines: BZP • Quipazine; Tryptamines: 2-Methyl-5-HT • 5-CT; Others: Chlorophenylbiguanide • RS-56812 • SR-57,227 • SR-57,227-A • YM-31636 Antagonists: Antiemetics: Alosetron • Azasetron • Batanopride • Bemesetron • Cilansetron • Dolasetron • Granisetron • Lerisetron • Ondansetron • Palonosetron • Ramosetron • Renzapride • Tropisetron • Zacopride • Zatosetron; Atypical Antipsychotics: Clozapine • Olanzapine • Quetiapine; Tetracyclic Antidepressants: Amoxapine • Mianserin • Mirtazapine; Others: BRL-46,470 • ICS-205,930 • Lu AA21004 • MDL-72,222 • Memantine 5-HT4 Agonists: Gastroprokinetic Agents: Cisapride • CJ-033,466 • Metoclopramide • Mosapride • Prucalopride • PRX-03140 • Renzapride • RS-67506 • TD-5108 • Tegaserod • Zacopride; Others: 5-MT • BIMU-8 • RS-67333 Antagonists: GR-113,808 • GR-125,487 • L-Lysine • Piboserod • RS-39604 • RS-67532 • SB-203,186 5-HT5 5-HT5A Agonists: Lysergamides: Ergotamine • LSD; Tryptamines: 5-CT; Others: Valerenic Acid Antagonists: Asenapine • Dimebolin • Methiothepin • Ritanserin • SB-699,551 • SB-699,551-A 5-HT5B Agonists: Lysergamides: Ergotamine • LSD Antagonists: Methiothepin 5-HT6 Agonists: Lysergamides: Lisuride • LSD • Metergoline; Tryptamines: 5-CT • 5-MT • E-6801 • E-6837 • EMD-386,088 • EMDT • LY-586,713 • WAY-181,187 • WAY-208,466 Antagonists: Antidepressants: Amitriptyline • Amoxapine • Clomipramine • Doxepin • Mianserin • Nortriptyline; Atypical Antipsychotics: Aripiprazole • Asenapine • Clozapine • Fluperlapine • Iloperidone • Olanzapine • Tiospirone; Typical Antipsychotics: Chlorpromazine • Loxapine; Others: BGC20-760 • BVT-5182 • BVT-74316 • Dimebolin • EGIS-12233 • GW-742,457 • Ketanserin • Methiothepin • MS-245 • PRX-07034 • Ritanserin • Ro 04-6790 • Ro 63-0563 • SB-258,585 • SB-271,046 • SB-357,134 • SB-399,885 5-HT7 Agonists: Lysergamides: LSD; Tryptamines: 5-CT • 5-MT; Others: 8-OH-DPAT • AS-19 • Bifeprunox • LP-12 • LP-44 • Sarizotan Antagonists: Antidepressants: Amitriptyline • Amoxapine • Clomipramine • Imipramine • Maprotiline • Mianserin; Atypical Antipsychotics: Amisulpride • Aripiprazole • Clozapine • Olanzapine • Risperidone • Sertindole • Tiospirone • Ziprasidone • Zotepine; Typical Antipsychotics: Chlorpromazine • Loxapine; Others: EGIS-12233 • LY-215,840 • Mesulergine • Metergoline • Methiothepin • Pimozide • Ritanserin • SB-258,719 • SB-258,741 • SB-269,970 • SB-656,104 • SB-656,104-A • SB-691,673 • SLV-313 • SLV-314 • Spiperone • SSR-181,507 Reuptake Inhibitors Plasmalemmal SERT Inhibitors Selective Serotonin Reuptake Inhibitors (SSRIs): Citalopram • Dapoxetine • Escitalopram • Fluoxetine • Fluvoxamine • Paroxetine • Sertraline • Vilazodone • Zimelidine; Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs): Bicifadine • Desvenlafaxine • Duloxetine • Milnacipran • Venlafaxine; Serotonin-Norepinephrine-Dopamine Reuptake Inhibitors (SNDRIs): Brasofensine • Diclofensine • DOV 102,677 • DOV 21,947 • DOV 216,303 • NS2359 • SEP-225289 • SEP-227162 • Tesofensine; Tricyclic Antidepressants (TCAs): Amitriptyline • Butriptyline • Cianopramine • Clomipramine • Desipramine • Dosulepin • Doxepin • Imipramine • Lofepramine • Nortriptyline • Protriptyline • Trimipramine; Tetracyclic Antidepressants (TeCAs): Amoxapine; Piperazines: Lubazodone • Nefazodone • Trazodone • Vilazodone; Tropanes: Cocaine; Antihistamines: Brompheniramine • Chlorpheniramine • Diphenhydramine • Pheniramine; Opioids: Meperidine/Pethidine • Methadone • Propoxyphene • Tramadol; Others: Cyclobenzaprine • Dextromethorphan • Mesembrine • SB-649915 • Sibutramine • Ziprasidone TRPC6 Activators Adhyperforin • Hyperforin Vesicular VMAT Inhibitors Ibogaine • Reserpine • Tetrabenazine Releasing Agents Aminoindanes: ETAI • MDAI • MDMAI • MMAI • TAI; Aminopropanes: Indanylaminopropane • Naphthylaminopropane; Benzofurans: 5-APDB; Oxazolines: 4-Methylaminorex • Aminorex; Phenethylamines: 2-Methyl-MDA • 3-Methoxy-4-methylamphetamine • 4-Bromomethcathinone • 4-Fluoroamphetamine • 4-Fluoromethamphetamine • 4-Methylamphetamine • 4-Methylmethamphetamine • 4-Methylthioamphetamine • 5-Methyl-MDA • BDB • BOH • Butylone • Chlorphentermine • Diethylcathinone • Dimethylcathinone • EBDB • Ethylone • Fenfluramine • Flephedrone • MBDB • MDA • MDEA • MDMA (Ecstasy) • MDOH • MDPEA • Mephedrone • Methylone • MMDA • MMDMA • Norfenfluramine • para-Bromoamphetamine • para-Chloroamphetamine • para-Chloromethamphetamine • para-Iodoamphetamine • para-Methoxyamphetamine • para-Methoxymethamphetamine • para-Methoxyethylamphetamine; Tryptamines: α-ET • α-MT Enzyme Inhibitors Anabolism TPH Inhibitors AGN-2979 • Fenclonine AAAD Inhibitors Benserazide • Carbidopa Catabolism MAO Inhibitors Nonselective: Iproclozide • Iproniazid • Isocarboxazid • Nialamide • Phenelzine • Pheniprazine • Tranylcypromine; MAO-A Selective: Befloxatone • Brofaromine • Cimoxatone • Clorgiline • Harmala Alkaloids • Minaprine • Moclobemide • Pirlindole • Toloxatone • Tyrima Others Precursors L-Tryptophan • 5-HTP Cofactors Iron • Tetrahydrobiopterin • Vitamin B3 (Niacin/Nicotinamide/NADPH) • Vitamin B6 (Pyridoxine/Pyridoxamine/Pyridoxal 5-Phosphate) • Vitamin B9 (Folic Acid/Tetrahydrofolic Acid) • Vitamin C (Ascorbic Acid) • Zinc Others Activity Enhancers: BPAP • PPAP; Reuptake Enhancers: Tianeptine

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