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| == '''What is Aprepitant?''' == | | {{#invoke:navbox|navbox |
| * Aprepitant ('''Emend''') is '''a substance P/neurokinin 1 (NK1) receptor antagonist''' used with other drugs to prevent nausea and vomiting caused by [[chemotherapy]]. It is also used to prevent nausea and vomiting after surgery.
| | | name = Anxiolytics |
| [[File:Aprepitant.svg|Aprepitant|thumb]] | | | title = [[Anxiolytic]]s ([[ATC code N05#N05B|N05B]]) |
| [[File:Aprepitant 3D ball.png|Aprepitant|thumb]]
| | | state = {{{state<includeonly>|collapsed</includeonly>}}} |
| == '''What are the uses of this medicine?''' == | | | groupstyle = text-align:center; |
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| Aprepitant ('''Emend''') is a prescription medicine used:
| | | group1 = {{abbrlink|5-HT<sub>1A</sub>R|5-HT1A receptor}} [[agonist]]s |
| * with other medicines that treat nausea and vomiting in patients 12 years of age and older to prevent nausea and vomiting caused by certain anti-cancer ([[chemotherapy]]) medicines | | | list1 = |
| * In adults to prevent nausea and vomiting after surgery | | * [[Buspirone]] |
| | * [[Gepirone]] |
| | * [[Tandospirone]] |
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| '''Limitations of use:''' | | | group2 = {{abbrlink|GABA<sub>A</sub>R|GABAA receptor}} {{abbrlink|PAMs|positive allosteric modulators}} |
| * Aprepitant capsules are not used to treat nausea and vomiting that you already have. | | | list2 = |
| * Aprepitant capsules should not be used continuously for a long time (chronic use). | | * ''[[Benzodiazepine]]s:'' [[Adinazolam]] |
| | * [[Alprazolam]] |
| | * [[Bromazepam]] |
| | * [[Camazepam]] |
| | * [[Chlordiazepoxide]] |
| | * [[Clobazam]] |
| | * [[Clonazepam]] |
| | * [[Clorazepate]] |
| | * [[Clotiazepam]] |
| | * [[Cloxazolam]] |
| | * [[Diazepam]]<sup>#</sup> |
| | * [[Ethyl loflazepate]] |
| | * [[Etizolam]] |
| | * [[Fludiazepam]] |
| | * [[Halazepam]] |
| | * [[Ketazolam]] |
| | * [[Lorazepam]]<sup>#</sup> |
| | * [[Medazepam]] |
| | * [[Nordazepam]] |
| | * [[Oxazepam]] |
| | * [[Pinazepam]] |
| | * [[Prazepam]]; ''Others:'' [[Alpidem]]<sup>‡</sup> |
| | * [[Barbiturate]]s (e.g., [[phenobarbital]]) |
| | * [[Carbamate]]s (e.g., [[meprobamate]]) |
| | * [[Carisoprodol]] |
| | * [[Chlormezanone]]<sup>‡</sup> |
| | * [[Alcohol (drug)|Ethanol (alcohol)]] |
| | * [[Etifoxine]] |
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| == '''How does this medicine work?''' == | | | group3 = [[Hypnotic]]s |
| | | list3 = |
| | * [[Zopiclone]] |
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| * Aprepitant (a pre’ pi tant) is a complex molecule with a central morpholine core and two ring carbons and fluorinated phenyl groups.
| | | group4 = [[Gabapentinoid]]s<br /><span style="font-size:85%;">([[Voltage-dependent calcium channel#.CE.B12.CE.B4_Subunit|{{abbr|α<sub>2</sub>δ|alpha2delta subunit}} {{abbr|VDCC|voltage-dependent calcium channel}}]] [[channel blocker|blocker]]s)</span> |
| * Aprepitant acts '''as a substance P antagonist blocking the neurokinin 1 (NK1) receptor, which is found in the central nervous system and induces the vomiting reflex when activated by substance P'''. | | | list4 = |
| * Aprepitant has been shown to '''inhibit both acute and delayed nausea and vomiting associated with cancer chemotherapy''' and surgical procedures. | | * [[Gabapentin]] |
| * It appears to act '''synergistically with serotonin type 3 (5-HT3) receptor blockers'''. | | * [[Gabapentin enacarbil]] |
| | * [[Phenibut]] |
| | * [[Pregabalin]] |
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| == '''Who Should Not Use this medicine ?''' == | | | group5 = [[Antidepressant]]s |
| | | list5 = |
| | * {{abbrlink|SSRIs|Selective serotonin reuptake inhibitors}} (e.g., [[escitalopram]]) |
| | * {{abbrlink|SNRIs|Serotonin-norepinephrine reuptake inhibitors}} (e.g., [[duloxetine]]) |
| | * {{abbrlink|SARIs|Serotonin antagonist and reuptake inhibitors}} (e.g., [[trazodone]]) |
| | * {{abbrlink|TCAs|Tricyclic antidepressants}} (e.g., [[clomipramine]]<sup>#</sup>) |
| | * {{abbrlink|TeCAs|Tetracyclic antidepressants}} (e.g., [[mirtazapine]]) |
| | * {{abbrlink|MAOIs|Monoamine oxidase inhibitors}} (e.g., [[phenelzine]]); ''Others:'' [[Agomelatine]] |
| | * [[Bupropion]] |
| | * [[Tianeptine]] |
| | * [[Vilazodone]] |
| | * [[Vortioxetine]] |
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| This medicine cannot be used in patients with:
| | | group6 = [[Antipsychotic]]s |
| * are allergic to aprepitant or any of the ingredients in aprepitant capsules. | | | list6 = |
| * are taking [[pimozide]] | | * [[Quetiapine]] |
| | * [[Flupentixol]] |
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| == '''What drug interactions can this medicine cause?''' ==
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| * Aprepitant capsules may affect the way other medicines work, and other medicines may affect how aprepitant capsules work causing serious side effects.
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| * Efficacy of [[contraceptives]] may be reduced during administration of and for 28 days following the last dose of aprepitant. Use effective alternative or back-up methods of contraception.
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| * Aprepitant is contraindicated with [[Pimozide]].
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| == '''Is this medicine FDA approved?''' == | | | group7 = [[Sympatholytic]]s<br /><span style="font-size:85%;">([[Antiadrenergic]]s)</span> |
| | | list7 = |
| | * [[Alpha-1 blocker]]s (e.g., [[prazosin]]) |
| | * [[Alpha-2 agonist]]s (e.g., [[clonidine]], [[dexmedetomidine]], [[guanfacine]]) |
| | * [[Beta blocker]]s (e.g., [[propranolol]]) |
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| * Aprepitant was approved for use in the United States in 2003 and current indications include prevention of [[postoperative]] and [[chemotherapy]] associated nausea and vomiting. | | | group8 = Others |
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| | | list8 = |
| == '''How should this medicine be used?''' ==
| | * [[Benzoctamine]] |
| | * [[Cycloserine]] |
| | * [[Fabomotizole]] |
| | * [[Hydroxyzine]] |
| | * [[Lorpiprazole]] |
| | * [[Mebicar]] |
| | * [[Mepiprazole]] |
| | * [[Nicotine]] |
| | * [[Opipramol]] |
| | * [[Oxaflozane]]<sup>‡</sup> |
| | * [[Phenaglycodol]] |
| | * [[Phenibut]] |
| | * [[Picamilon]] |
| | * [[Selank]] |
| | * [[Tiagabine]] |
| | * [[Tofisopam]] |
| | * [[Validolum]] |
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| '''Recommended dosage:'''
| | | list9 = {{PharmNavFootnote}} |
| '''For Prevention of Chemotherapy Induced Nausea and Vomiting (CINV):'''
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| * Aprepitant capsules in adults and pediatric patients 12 years of age and older: is 125 mg on Day 1 and 80 mg on Days 2 and 3.
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| * Administer aprepitant 1 hour prior to chemotherapy on Days 1, 2, and 3.
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| * If no chemotherapy is given on Days 2 and 3, administer aprepitant in morning.
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| '''For postoperative nausea and vomiting (PONV):'''
| | }}<noinclude> |
| * Adults: 40 mg aprepitant capsules within 3 hours prior to induction of anesthesia.
| | {{collapsible option}} |
| | | [[Category:Drug_templates by ATC]] |
| '''Administration:'''
| | </noinclude> |
| * Swallow aprepitant capsules whole.
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| * Aprepitant capsules may be taken with or without food.
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| * If you take too much aprepitant, call your healthcare provider, or go to the nearest hospital emergency room.
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| * Aprepitant capsules are taken as 3 doses over 3 days - starting on the day you have chemotherapy, and for the following 2 days.
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| In adults, your healthcare provider may prescribe aprepitant capsules for you:
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| * Capsules of aprepitant by mouth for all 3 doses:
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| * You should get a package that has 3 capsules of aprepitant.
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| * Day 1 (Day of [[chemotherapy]]): Take one 125 mg capsule of aprepitant (white and pink) by mouth 1 hour before you start your chemotherapy treatment.
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| * Day 2 and Day 3: Take one 80 mg capsule of aprepitant (white) by mouth 1 hour before you start your chemotherapy treatment. If no chemotherapy treatment is given on Days 2 and 3, aprepitant capsules should be taken in the morning.
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| In children 12 years of age and older who can swallow capsules by mouth, aprepitant is prescribed as capsules of aprepitant by mouth for all 3 doses:
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| * You should get a package that has 3 capsules of aprepitant capsules.
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| * Day 1 (Day of chemotherapy): Take one 125 mg capsule of aprepitant capsules (white and pink) by mouth 1 hour before you start your chemotherapy treatment.
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| * Day 2 and Day 3: Take one 80 mg capsule of aprepitant (white) by mouth 1 hour before you start your chemotherapy treatment. If no chemotherapy treatment is given on Days 2 and 3, aprepitant should be taken in the morning.
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| If you are an adult and are having surgery:
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| * Your doctor will prescribe a 40 mg capsule of aprepitant for you before surgery. Take aprepitant within 3 hours before surgery.
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| * Follow your healthcare provider’s instructions about restrictions on eating and drinking before surgery.
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| * If you take the blood thinner medicine [[warfarin sodium]] (COUMADIN®, JANTOVEN®), your healthcare provider may do blood tests after you take aprepitant capsules to check your blood clotting.
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| == '''What are the dosage forms and brand names of this medicine?''' ==
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| This medicine is available in fallowing doasage form:
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| * '''As Aprepitant Capsules, USP:''' 40 mg; 80 mg; 125 mg
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| This medicine is available in fallowing brand namesː
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| * '''Emend'''
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| =='''What side effects can this medication cause?'''==
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| The most common side effects of this medicine include:
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| '''For Prevention of Chemotherapy Induced Nausea and Vomiting (CINV):'''
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| '''In adults:'''
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| * tiredness, [[diarrhea]], weakness, indigestion, stomach (abdominal) pain, hiccups, decrease in [[white blood cell]] count, dehydration, and changes in liver function tests.
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| '''For postoperative nausea and vomiting (PONV):'''
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| '''In adults:'''
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| * constipation and low blood pressure ([[hypotension]])
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| '''In children 6 months to 17 years of age:'''
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| * decrease in white blood cell count, headache, [[diarrhea]], decreased appetite, cough, tiredness, decrease in red blood cell count, dizziness, and [[hiccups]]
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| ==''' What special precautions should I follow?''' ==
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| * Instruct patients on chronic [[warfarin]] therapy to follow instructions from their healthcare provider regarding blood draws to monitor their INR during the 2-week period, particularly at 7 to 10 days, following initiation of the 3-day regimen of aprepitant with each chemotherapy cycle, or following administration of a single 40-mg dose of aprepitant for the prevention of [[postoperative nausea and vomiting]].
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| * Advise patients that administration of aprepitant may reduce the efficacy of [[hormonal contraceptives]]. Instruct patients to use effective alternative or back-up methods of [[contraception]] (such as condoms and [[spermicides]]) during treatment with aprepitant and for 1 month following the last dose of aprepitant.
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| * [[Hypersensitivity]] reactions, including [[anaphylaxis]], have been reported in patients taking aprepitant. Advise patients to stop taking aprepitant and seek immediate medical attention if they experience signs or symptoms of a hypersensitivity reaction, such as [[hives]], rash and itching, skin peeling or sores, or difficulty in breathing or swallowing.
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| == '''What to do in case of emergency/overdose?''' ==
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| Symptoms of overdosage may include:
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| * [[Drowsiness]] and headache
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| '''Management of overdosage:'''
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| * In the event of overdose, aprepitant should be discontinued and general supportive treatment and monitoring should be provided.
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| * Because of the [[antiemetic]] activity of aprepitant, drug-induced [[emesis]] may not be effective in cases of aprepitant overdosage.
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| * Aprepitant is not removed by [[hemodialysis]].
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| == '''Can this medicine be used in pregnancy?''' ==
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| * It is not known if aprepitant capsules can harm your unborn baby.
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| * Women who use birth control medicines containing hormones to prevent pregnancy ([[birth control pills]], skin patches, [[implants]], and certain IUDs) should also use a back-up method of birth control that does not contain hormones, such as [[condoms]] and [[spermicides]], during treatment with aprepitant capsules and for 1 month after your last dose of aprepitant capsules.
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| =='''Can this medicine be used in children?'''==
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| * The safety and effectiveness of aprepitant for the prevention of nausea and vomiting associated with HEC or MEC have not been established in patients less than 6 months.
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| * The safety and effectiveness of aprepitant have not been established for the prevention of postoperative nausea and vomiting in pediatric patients.
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| == '''What are the active and inactive ingredients in this medicine?''' ==
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| * '''Active ingredient:''' aprepitant
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| * '''Inactive ingredients:''' colloidal silicon dioxide, hydroxyethyl cellulose, microcrystalline cellulose, mannitol, poloxamer, povidone, sodium stearyl fumarate, vitamin E polyethylene glycol succinate, and purified water. The capsule shell excipients are gelatin, sodium lauryl sulphate and titanium dioxide. The 40-mg capsule shell also contains iron oxide yellow, and the 125-mg capsule also contains FD&C Red #3. Non-volatile solvents in the imprinting ink are shellac, iron oxide black and potassium hydroxide.
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| == '''Who manufactures and distributes this medicine?''' ==
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| '''Manufactured by:'''
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| * [[Glenmark Pharmaceuticals Limited]]
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| * Plot No. 2, Phase-2, Pharma Zone SEZ
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| * Pithampur, Dist.-Dhar
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| * Madhya Pradesh, India
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| '''Manufactured for:'''
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| * [[Glenmark Pharmaceuticals Inc., USA|Glenmark Pharmaceuticals Inc.]], USA
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| * Mahwah, NJ
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| == '''What should I know about storage and disposal of this medication?''' ==
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| * Store at room temperature, between 68°F to 77°F (20°C to 25°C).
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| {{Antidepressants}}
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| {{Anxiolytics}}
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| {{Portal bar|Medicine}} | |
| [[Category:Antiemetics]] | |
| [[Category:Fluoroarenes]]
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| [[Category:Lactams]]
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| [[Category:Merck & Co. brands]]
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| [[Category:Morpholines]]
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| [[Category:NK1 receptor antagonists]]
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| [[Category:Triazoles]]
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| [[Category:Trifluoromethyl compounds]]
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| [[Category:Ureas]]
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| [[Category:World Health Organization essential medicines]]
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| {{gastrointestinal agents}}
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