Escitalopram apollo

Transcription

1 Escitalopram apollo Escitalopram apollo Escitalopram CAS Number : Molecular Formula : C20H21FN2O Molecular Weight : g/mol Systematic (IUPAC) : (1S)-1-[3- (dimethylamino)propyl]-1-(4-fluorophenyl)-1,3- dihydro-2-benzofuran-5-carbonitrile

2 Type : small molecule Description Escitalopram, the S-enantiomer of citalopram, belongs to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Despite distinct structural differences between compounds in this class, SSRIs possess similar pharmacological activity. As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine reuptake and do not antagonize α- or β-adrenergic, dopamine D2 or histamine H1 receptors. During acute use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT1A and terminal autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to enhanced serotonergic neurotransmission. Side effects include dry mouth, nausea, dizziness, drowsiness, sexual dysfunction and headache. Side effects generally occur within the first two weeks of therapy and are usually less severe and frequent than those observed with tricyclic antidepressants. Escitalopram may be used to treat major depressive disorder (MDD) and generalized anxiety disorder (GAD). Categories Serotonin Uptake Inhibitors Antidepressive Agents, Second-Generation

3 Taxonomy Kingdom : Organic Classes Benzofurans Benzyl Alcohols and Derivatives Nitriles and Derivatives Substructures Benzofurans Benzyl Alcohols and Derivatives Nitriles and Derivatives Ethers Benzene and Derivatives Cyanides Aliphatic and Aryl Amines Halobenzenes Heterocyclic compounds Aromatic compounds Aryl Halides Pharmacology Indication : Labeled indications include major depressive disorder (MDD) and generalized anxiety disorder (GAD). Unlabeled indications include treatment of mild dementia-associated agitation in nonpsychotic patients. Pharmacodynamics : Escitalopram is one of a class of antidepressants known as selective serotonin reuptake

4 inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessivecompulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. In vitro studies show that escitalopram is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Escitalopram has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of escitalopram was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Escitalopram does not inhibit monoamine oxidase. Mechanism of action : The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Escitalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs.

5 Absorption : The absolute bioavailability of citalopram is about 80% relative to an intravenous dose. Volume of distribution : 12 L/kg Protein binding : ~56% Metabolism : Mainly hepatic. Escitalopram undergoes N-demethylation to S-demethylcitalopram (S-DCT) and S-didemethylcitalopram (S-DDCT). CYP3A4 and CYP2C19 are the enzymes responsible for this N- demethylation reaction. Route of elimination : Following oral administrations of escitalopram, the fraction of drug recovered in the urine as escitalopram and S-demethylcitalopram (S- DCT) is about 8% and 10%, respectively. The oral clearance of escitalopram is 600 ml/min, with approximately 7% of that due to renal clearance. Escitalopram is metabolized to S-DCT and S- didemethylcitalopram (S-DDCT). Half life : hours Clearance : oral cl=600 ml/min Toxicity : Signs of overdose include convulsions, coma, dizziness, hypotension, insomnia, nausea, vomiting, sinus tachycardia, somnolence, and ECG changes (including QT prolongation).

6 Affected organisms : Humans and other mammals Drug Class And Mechanisms Escitalopram is an oral drug that is used for treating depression and generalized anxiety disorder. Chemically, escitalopram is similar to citalopram (Celexa). Both are in the class of drugs called selective serotonin reuptake inhibitors (SSRIs), a class that also includes fluoxetine (Prozac), paroxetine (Paxil) and sertraline (Zoloft). SSRIs work by affecting neurotransmitters in the brain, the chemical messengers that nerves use to communicate with one another. Neurotransmitters are made and released by nerves and then travel to other nearby nerves where they attach to receptors on the nerves. Some neurotransmitters that are released do not bind to receptors and are taken up by the nerves that produced them. This is referred to as "reuptake." Many experts believe that an imbalance of neurotransmitters is the cause of depression. Escitalopram prevents the reuptake of one neurotransmitter, serotonin, by nerves, an action which results in more serotonin in the brain to attach to receptors. The FDA approved escitalopram in August Uses Escitalopram is an antidepressant (selective serotonin reuptake inhibitor-ssri) used to treat depression and anxiety. It works by restoring the balance of certain natural substances (neurotransmitters such as serotonin) in the brain. Escitalopram may improve your feelings of well-being and energy level and decrease nervousness.other This section contains uses of this

7 drug that are not listed in the approved US professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.this medication may also be used to treat other mental/mood disorders (such as obsessive-compulsive disorder, panic disorder). How To Use? Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start taking escitalopram and each time you get a refill. If you have any questions, ask your doctor or pharmacist.take this medication by mouth with or without food as directed by your doctor, usually once daily in the morning or evening. Take it at the same time each day. The dosage is based on your medical condition and response to treatment. If you are using the liquid form of this medication, carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose.to reduce your risk of side effects, your doctor may direct you to start taking this drug at a low dose and gradually increase your dose. Follow your doctor's instructions carefully. Do not take more or less medication or take it more frequently than prescribed. Your condition will not improve any faster, and your risk of side effects will increase.it is important to continue taking this medication even if you feel well. Do not stop taking this medication without consulting your doctor. Some conditions may become worse when the drug is suddenly stopped. Your dose may need to be gradually

8 decreased.this medication may cause withdrawal reactions, especially if it has been used regularly for a long time or in high doses. In such cases, withdrawal symptoms (such as nervousness, headache, numbness, tingling, trouble sleeping, confusion) may occur if you suddenly stop using this medication. To prevent withdrawal reactions, your doctor may reduce your dose gradually. Consult your doctor or pharmacist for more details, and report any withdrawal reactions immediately.it may take 1 to 2 weeks to feel a benefit from this drug and 4 weeks to feel the full benefit of this medication. Tell your doctor if your condition persists or worsens. Dosing The usual starting dose of escitalopram is 10 mg once daily in the morning or evening. The dose may be increased to 20 mg once daily after 1 week. Benefit may not be seen until treatment has been given for up to 4 weeks. A daily dose of 20 mg may not be anymore effective than 10 mg daily for treatment of depression. Escitalopram can be taken with or without food. Drug Interactions All SSRIs, including escitalopram, should not be combined with drugs in the monoamine oxidase (MAO) inhibitor class of antidepressants such as isocarboxazid (Marplan), phenelzine (Nardil), tranylcypromine (Parnate), selegiline (Eldepryl) and procarbazine (Matulane). Such combinations may lead to confusion, high blood pressure, high fevers, tremor or muscle rigidity, and increased activity. At least 14 days should elapse after discontinuing escitalopram before starting

9 an MAO inhibitor. Conversely, at least 14 days should elapse after discontinuing an MAO inhibitor before starting escitalopram. Side Effects Nausea, dry mouth, trouble sleeping, constipation, tiredness, drowsiness, dizziness, or increased sweating may occur. If any of these effects persist or worsen, tell your doctor promptly.remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.tell your doctor immediately if any of these unlikely but serious side effects occur: unusual or severe mental/mood changes (such as confusion, difficulty concentrating, nervousness, unusual high energy/excitement, rare thoughts of suicide), decreased interest in sex, changes in sexual ability.tell your doctor immediately if any of these rare but serious side effects occur: easy bruising/bleeding, muscle weakness/cramps, change in the amount of urine.get medical help right away if any of these rare but serious side effects occur: bloody/black/tarry stools, fainting, vomit that looks like coffee grounds, seizures.this medication may rarely cause a very serious condition called serotonin syndrome. The risk increases when this medication is used with certain other drugs (see Drug Interactions section). Get medical help right away if you develop some of the following symptoms: hallucinations, unusual restlessness, loss of coordination, fast heartbeat, severe dizziness, unexplained fever, severe nausea/vomiting/diarrhea, twitching muscles.rarely, males may have a painful or prolonged erection lasting 4

10 or more hours. If this occurs, stop using this drug and get medical help right away, or permanent problems could occur.a very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.this is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist. Precautions Before taking escitalopram, tell your doctor or pharmacist if you are allergic to it; or to citalopram; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.before using this medication, tell your doctor or pharmacist your medical history, especially of: personal or family history of psychiatric disorders (such as bipolar/manic-depressive disorder), personal or family history of suicide attempts, bleeding problems, liver disease, seizures, kidney disease, stomach bleeding (such as ulcers), severe loss of body water (dehydration), low sodium in the blood (hyponatremia).this drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Avoid alcoholic beverages.before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).older adults may be more sensitive to the effects of this drug. They may be more likely to

11 lose too much salt (hyponatremia), especially if they are also taking "water pills" (diuretics) with this medication.during pregnancy, this medication should be used only when clearly needed. It may harm an unborn baby. Also, babies born to mothers who have used this drug during the last 3 months of pregnancy may infrequently develop withdrawal symptoms such as feeding/breathing difficulties, seizures, muscle stiffness, or constant crying. If you notice any of these symptoms in your newborn, tell the doctor promptly.since untreated depression can be a serious condition, do not stop using this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately discuss with your doctor the benefits and risks of using this medication during pregnancy.this medication passes into breast milk and may have undesirable effects on a nursing infant. Consult your doctor before breastfeeding. Notes Do not share this medication with others.psychiatric/medical check-ups and possibly lab tests should be done periodically to monitor your progress or check for side effects. Consult your doctor for more details. Missed Dose If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

12 Storage Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product. apollo asia Division APOLLO Pharmaceuticals API Manufacturers INDIA [P] Ltd. asia Division Mr.Vipin Saxena CEO Cellular: Cellular: Direct : FAX : Wireline Purchase HELPDESK: Wireline Sales HELPDESK: Wireless 24x7 HELPDESK: Blackberry Pin : 32E6500D 32E C58

13 Chat: MSN Hotmail:VipinrSaxena Skype NAME:VipinrSaxena Rocketmail:VipinrSaxena Google mail:vipinrsaxena BlackBerry:28415C58 Regd. Office :- 1104, Maker Chamber V, Nariman Point Mumbai, INDIA Pin: Industrial Office D-62, OIC India Oshiwara Industrial Centre, New Link Road, Goregoan West, Mumbai, INDIA Pin: Manufacturing Unit Address: Plot No. 117A, Village: Chamble Near MonaTona Limited.Wada, Maharashtra, PIN : INDIA

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