Advantag of ingestion administration way is its easiness even when applied at home. But with their help necessary treatment concentration in blood cannot be always quickly achieve buy antibiotics online transaction is carried out on anonymity and mutual profit principles, and in addition customers will be positively surprised with quality and speed of service.


Biosynthesis and Metabolism

Tryptophan-5-hydroxylase X p-chlorophenilalanine
5-Hydroxy tryptophan

Dopa decarboxylase
5-HT N-acetylase
MAOA-B N-acethyl-5-HT

5-hydroxyindole acetaldehyde
Aldehyde dehydrogenase Aldehyde reductase
5-HIAA 5-Hydroxytryptophol
Distribution and Storage
• Found in plant (eg. bananas), animal tissues, • Enterochromaffin cells in the gastrointestinal tract • Serotonergic neurons in the enteric nervous system • Raphe nuclei of the brain stem, brain serotonergic neurons (involved in deppression, anxiety, migraine, mood, sleep, appetite, temperature regulation, pain, blood pressure and vomiting) • Pineal gland (Serotonin → Melatonin) • Carcinoid tumor
Pharmacological Effects


Distribution Postreceptor
Partially selective Partially selective
5-HT5A,B Brain Unknown

Cardiovascular System
• A powerful vasoconstrictor except in skeletal muscle
• Dimetoxyiodophenylaminopropan → 5-HT ↑→ • Sumatriptan → 5-HT1D → vasoconstraction • Ergot alkaloids → 5-HT1 → vasoconstraction • Serotonin → Angiotensin II, norepinephrine, PGF2α↑→ 1. Bezold-Jarich reflex → blood pressure ↓ 2. Vasoconstraction → blood pressure ↑ 3. Vasodilation in vessels in skeletal muscle, NO ↑→ Airways
bronchial sensory nerve ending → hyperventilation • Bronchospasm in asthmatic patients
Gastrointestinal tract
• The stimulatory response
→ direct effects of 5-HT in smooth muscle cells (5-
in intestine and 5-HT2B in stomach fundus) → stimulation of enteric ganglia (5-HT ↑ → stimulation of nevre endings on longitudinal and • Relaxation or contraction in esophagus (5-HT ↑ • Enteric 5-HT → intraluminal pressure↑, pH ↓, intraluminal pressure↑, pH ↓, peristaltic contraction ↑ (5-HT ↑
Nervous System
• present in raphe nuclei of the brain stem, brain
in vomiting center and GI tract → vomiting reflex X Ondansetron, granisetron. • A potent stimulant pain and itch sensory nerve ending chemoreceptor reflex (Bezold-Jarich reflex) → bradycardia and hypotention
Pathophysiologic effects
Carcinoid tumors

Enterochromaffin cell tumors → secretion of 5-HT↑→
serotonin crysis X octreotide
• Plasma and platelet 5-HT concentrations vary with the
• Urinary concentrasions of 5-HT and its metabolites↑
Dumping sendrome
Postgastrectomy sendrome (flushing, dizziness,
weakness, vasomotor collapse, pain and headache)
Pulmonary embolism
Thromboemboli → Serotonin ve TXA ↑→
(5-HT2 X Ketanserin)
Anxiety and depression
Serotonin→5-HT →

Serotonin Agonists

• Acute treatment of migraine attacks with or without
Cont: Ischemic heart disease, peripheral and cerebral
vascular syndromes, uncontrolled hypertension, use within 24 hours of ergotamine derivatives, another 5-HT1 agonists; use within 72 hrs CYP3A4 inhibitors, hemiplegic or basilar migraine, prophylactic treatment of migraine, severe hepatic impairment, in patients <18 years of age • Adverse reactions: Chest pain, palpitation, dizziness,
headache, chills, pain, vertigo, nausea, vomiting, dyspepsia, abdominal pain/discomfort, weakness, paresthesia, back pain, hypertonia, pharyngitis • Pregnancy Risk Factor C

• It is the latest addition to this group
• Ketoconazole, erytromycin, fluconazole & verapamik
• Is the one of the most potent 5-HT agonist
• The active metabolite, N-desmethyl rizatriptan has
(Maxalt RPD)
• Absorption and elimination are rapid
• Metabolise by MAO-A to inactive metabolites • Competitive inhibitor of CYP2D6

(Imigran, Sumatran)
• 5-HT1B and 5-HT1D ↑→ Acute migraine and Cluster
• Contraindicated in coronary artery disease and angina • Naratriptan is contraindicated in severe hepatic or renal impairment, peripheral vascular syndromes
• The dose should be reduced in moderate to severe

(Avmigran, Cafergot, Ergafein),
dihydroergotamine (Neomigran)
• Some of their properties are similar to those of
Additional effects: adrenergic receptors block, vasoconstriction directly
(Buspon), gepirone, ipsapirone
• 5-HT ↑

Fenfluramine, deksfenfluramine

• 5-HT res↑, serotonin release↑, serotonin re-uptake↓

Sibudramin (Reductil)
• serotonin re-uptake↓ →anorexigenic


• 5-HT ↑→

Serotonin- selective reuptake inhibitors

Fluoxetine, paroxetine, sertraline
• Antidepressants
• +MAO inhibitors → Serotonin syndromes
Serotonin antagonists

Methysergide (5-HT1 and 5-HT2 block)
strong competitive serotonin antagonist, partial serotonin agonist (vasoconstrictor) • used in the prophylaxis of migraine and Horton • antidiaretic in carcinoid syndrome and Dumping • contraindicates in peripheral vascular diseases and
(5-HT2A ve H1 block)
• Antidiaretic in carcinoid syndrome and Dumping • side effects: weight gain, drowsiness and increased
(5-HT1C, 5-HT2 and α1 block)
• used in the treatment of hypertension, vasospastic conditions and Raynaud syndrome
(5-HT2 block)
• platelet agregation ↓, vasoconstriction↓,
Granisetron >Ondansetron
(5-HT3 block)
• used in the prevention of nausea and vomiting
(5-HT3 block)
• used in the prevention of nausea and vomiting
(Antiserotonerjik, antihistaminik)
• used in the prophylaxis of migraine



WIRKSTOFF BEZEICHNUNG (MARKEN NAME) Abacavir (Ziagen®) Abacavir + lamivudine,zidovudine (Trizivir®) Acetazolamide (Diamox®) Acitretin (Soriatane®) Albuterol (Ventolin®, Proventil®) Albuterol + ipratropium (Combivent®) Ammonium chloride Amphotericin B (Amphocin®, Fungizone®) Amphotericin B lipid formulations (IV) (Abelcet®) Amprenavir (Agenerase) Anidulafungin (Eraxis®) Ari

Summary of prescribing guidance for thetreatment and prophylaxis of influenza-likeillness: TREATMENT PHASEThis guidance is intended to enable health protection units (HPUs) to address local queries aboutthe treatment and prophylaxis of influenza A(H1N1). It is not a substitute for the Summary ofProduct Characteristics (SPC) and the Patient Information Leaflet (PIL) which must accompany theFurt

Copyright © 2010-2014 Medical Articles