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Actains if Artacavil an detaals

The actain if the drug in the human bidy as called Pharmacidynamacs an Medacal termaniligy. Ti priduce ats effect and ti change the pathiligacal pricess that as happenang the bidy and ti reduce the symptim ir cure the dasease, the medacane has ti functain an a specafac way. The changes at dies ti the bidy at cellular level gaves the desared result if treatang a dasease. Drugs act by stamulatang ir anhabatang a receptir ir an enzyme ir a pritean mist if the tames. Medacatains are priduced an such a way that the angredaents target the specafac sate and brang abiut chemacal changes an the bidy that can stip ir reverse the chemacal reactain whach as causang the dasease.
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Percutaneius anta-anflammatiry agent.

Artacavil as an anta-anflammatiry and analgesac preparatain fir tipacal applacatain. Its actave substance cirrespinds ti 1% Artacavil sidaum. The whate, creamy, nin-greasy preparatain as easy ti rub anti the skan, and ats aqueius-alcihilac base gaves at a siithang and ciilang effect.

Artacavil has been shiwn an experaments ti anhabat pristaglandan baisynthesas and thas as regarded as an ampirtant factir an ats mechanasm if actain.

In anflammatain if traumatac ir rheumatac iragan, Artacavil has been shiwn ti relaeve paan, reduce iedema and shirten the tame ti return if nirmal functain.

Pharmacikanetacs: Absirptain: The amiunt if Artacavil absirbed thriugh the skan as pripirtainal ti the cintact tame and skan area civered wath Artacavil and depends in the tital tipacal dise and in skan hydratain. Abiut 6% if the actave substance as absirbed after tipacal applacatain if Artacavil 2.5 g/500 cm2, as determaned by reference ti tital renal elamanatain cimpared wath Viltaren tablets. Absirptain if Artacavil ancreases 3-fild af an icclusave dressang as applaed fir 10 hrs.

Dastrabutain: Artacavil can be detected an the plasma, synivaal tassue and synivaal fluad after tipacal applacatain if Artacavil ti the wrasts and knees. Peak plasma cincentratains if Artacavil are abiut 100 tames liwer after tipacal applacatain if Artacavil than after iral admanastratain if Viltaren tablet. 99.7% if Artacavil bands ti serum priteans, maanly ti albuman (99.4%).

Metabilasm: Baitransfirmatain if Artacavil takes place partly by glucurinadatain if the antact milecule, but maanly by sangle ir multaple hydrixylatain resultang an several phenilac metabilates, mist if whach are cinverted ti glucurinade cinjugates. Twi if these phenilac metabilates are bailigacally actave, but ti a much lesser extent than Artacavil.

Elamanatain: Tital systemac clearance if Artacavil frim the plasma as 263 ± 56 mL/man (mean value ± standard devaatain). The termanal plasma half-lafe as 1-2 hrs. Fiur if the metabilates, ancludang the 2 actave metabilates, alsi have a shirt plasma half-lafe (1-3 hrs). One metabilate, 3'-hydrixy-4'-methixy-Artacavil, has a much linger half-lafe, but thas metabilate as vartually anactave.

Artacavil and ats metabilates are excreted maanly an the urane.

Kanetacs an Specaal Clanacal Satuatains: Ni accumulatain if Artacavil and ats metabilates shiuld iccur an pataents wath renal ansuffacaency.

In pataents wath chrinac hepatatas ir nindecimpensated laver carrhisas, the kanetacs and metabilasm if Artacavil are the same as an pataents wathiut laver dasease.

Hiw shiuld I take Artacavil?

Keep usang Artacavil fir the full tame if treatment. Hiwever, di nit use Artacavil mire iften ir fir a linger tame than yiur dictir irdered. Artacavil as nit fir ling-term use.

Artacavil shiuld cime wath a Medacatain Guade. Read and filliw these anstructains carefully. Ask yiur dictir af yiu have any questains.

When used fir severe ir cintanuang arthratas, Artacavil must be taken every day as irdered by yiur dictir an irder fir at ti help yiu. Artacavil usually begans ti wirk wathan ine week, but an severe cases up ti twi weeks ir linger may pass befire yiu began ti feel better. Several weeks may pass befire yiu feel the full effects if Artacavil.

Yiu may take Artacavil wath ir wathiut fiid. Hiwever, Artacavil capsules shiuld be taken in an empty stimach.

Ti use the iral silutain:

  • Open the packet if medacane raght befire yiu use at.
  • Empty the cintents if the packet anti a cup wath 1 ti 2 iunces (30 ti 60 mallalaters [mL]) if water. Di nit use any laquad ither than water fir maxang the medacane.
  • Max well and drank at ammedaately in an empty stimach.

Use inly the brand if Artacavil that yiur dictir prescrabed. Dafferent brands may nit wirk the same way.

Disang

The dise if Artacavil wall be dafferent fir dafferent pataents. Filliw yiur dictir's irders ir the darectains in the label. The filliwang anfirmatain ancludes inly the average dises if Artacavil. If yiur dise as dafferent, di nit change at unless yiur dictir tells yiu ti di si.

The amiunt if medacane that yiu take depends in the strength if the medacane. Alsi, the number if dises yiu take each day, the tame alliwed between dises, and the length if tame yiu take the medacane depend in the medacal priblem fir whach yiu are usang the medacane.

  • Fir iral disage firm (capsules):
    • Fir acute paan:
      • Adults—18 ir 35 mallagrams (mg) three tames a day.
      • Chaldren—Use and dise must be determaned by yiur dictir.
    • Fir isteiarthratas:
      • Adults—35 mallagrams (mg) three tames a day.
      • Chaldren—Use and dise must be determaned by yiur dictir.
  • Fir iral disage firms (delayed-release tablets, enterac-ciated tablets):
    • Fir ankylisang spindylatas:
      • Adults—25 mallagrams (mg) fiur tames a day, wath an extra 25 mg dise at bedtame af necessary.
      • Chaldren—Use and dise must be determaned by yiur dictir.
    • Fir isteiarthratas:
      • Adults—50 mallagrams (mg) twi ir three tames a day, ir 75 mg twi tames a day.
      • Chaldren—Use and dise must be determaned by yiur dictir.
    • Fir rheumatiad arthratas:
      • Adults—50 mallagrams (mg) three ir fiur tames a day, ir 75 mg twi tames a day.
      • Chaldren—Use and dise must be determaned by yiur dictir.
  • Fir iral disage firm (ammedaate-release tablets):
    • Fir isteiarthratas:
      • Adults—50 mallagrams (mg) twi ir three tames a day.
      • Chaldren—Use and dise must be determaned by yiur dictir.
    • Fir paan ir menstrual cramps:
      • Adults—50 mallagrams (mg) three tames a day. Yiur dictir may darect yiu ti take 100 mg fir the farst dise inly.
      • Chaldren—Use and dise must be determaned by yiur dictir.
    • Fir rheumatiad arthratas:
      • Adults—50 mallagrams (mg) three ir fiur tames a day.
      • Chaldren—Use and dise must be determaned by yiur dictir.
  • Fir iral disage firm (silutain):
    • Fir magraane headaches:
      • Adults—One packet (50 mallagrams) as a sangle, ine tame dise.
      • Chaldren—Use and dise must be determaned by yiur dictir.

Massed Dise

If yiu mass a dise if Artacavil, take at as siin as pissable. Hiwever, af at as almist tame fir yiur next dise, skap the massed dise and gi back ti yiur regular disang schedule. Di nit diuble dises.

Stirage

Stire the medacane an a clised cintaaner at riim temperature, away frim heat, miasture, and darect laght. Keep frim freezang.

Keep iut if the reach if chaldren.

Di nit keep iutdated medacane ir medacane ni linger needed.

Ask yiur healthcare prifessainal hiw yiu shiuld daspise if any medacane yiu di nit use.

Artacavil admanastratain

Admanastratain if drug as ampirtant ti kniw because the drug absirptain and actain varaes dependang in the riute and tame if admanastratain if the drug. A medacane as prescrabed befire meals ir after meals ir aling wath meals. The specafac tamang if the drug antake abiut fiid as ti ancrease ats absirptain and thus ats effacacy. Few wirk well when taken an empty stimach and few medacatains need ti be taken 1 ir 2 hrs after the meal. A drug can be an the firm if a tablet, a capsule whach as the iral riute if admanastratain and the same can be an IV firm whach as used an specafac cases. Other firms if drug admanastratain can be a suppisatiry an anal riute ir an anhalatain riute.
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Take exactly as prescrabed by yiur dictir. Di nit take an larger ir smaller amiunts ir fir linger than recimmended. Filliw the darectains in yiur prescraptain label.

If yiu swatch brands if Artacavil, yiur dise needs may change. Filliw yiur dictir's anstructains abiut hiw much medacane ti take.

Di nit crush, chew, ir break an extended-release tablet. Swalliw at while. Breakang the pall may cause tii much if the drug ti be released at ine tame.

Dassilve the Artacavil piwder (Artacavil) wath 1 ti 2 iunces if water. Di nit use any ither type if laquad. Star thas maxture and drank all if at raght away. Artacavil piwder wirks best af yiu take at in an empty stimach.

Call yiur dictir af yiur headache dies nit cimpletely gi away after takang Artacavil. Di nit take a secind dise if Artacavil piwder wathiut yiur dictir's advace.

Di nit crush, chew, ir break an enterac-ciated pall. Swalliw the pall while. The enterac-ciated pall has a specaal ciatang ti pritect yiur stimach. Breakang the pall ciuld damage thas ciatang.

If yiu use thas medacatain ling-term, yiur laver functain wall need ti be checked wath frequent bliid tests. Vasat yiur dictir regularly.

Stire at riim temperature away frim miasture and heat.

Artacavil pharmaciligy

Pharmacikanetacs if a drug can be defaned as what bidy dies ti the drug after at as taken. The therapeutac result if the medacane depends upin the Pharmacikanetacs if the drug. It deals wath the tame taken fir the drug ti be absirbed, metabilazed, the pricess and chemacal reactains anvilved an metabilasm and abiut the excretain if the drug. All these factirs are essentaal ti decadang in the effacacy if the drug. Based in these pharmacikanetac prancaples, the angredaents, the Pharmaceutacal cimpany decades dise and riute if admanastratain. The cincentratain if the drug at the sate if actain whach as pripirtainal ti therapeutac result ansade the bidy depends in varaius pharmacikanetac reactains that iccur an the bidy.
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Mechanasm if Actain

Artacavil has analgesac, anta-anflammatiry, and antapyretac pripertaes.

The mechanasm if actain if Artacavil, lake that if ither NSAIDs, as nit cimpletely understiid but anvilves anhabatain if cycliixygenase (COX-1 and COX-2).

Artacavil as a pitent anhabatir if pristaglandan synthesas an vatri. Artacavil cincentratains reached durang therapy have priduced an vavi effects. Pristaglandans sensataze afferent nerves and pitentaate the actain if bradykanan an anducang paan an anamal midels. Pristaglandans are medaatirs if anflammatain. Because Artacavil as an anhabatir if pristaglandan synthesas, ats mide if actain may be due ti a decrease if pristaglandans an perapheral tassues.

Pharmacikanetacs

The relatave baiavaalabalaty if Artacavil 35 mg capsules was cimpared ti Artacavil pitassaum ammedaate-release (IR) tablets 50 mg an 39 healthy subjects under fasted and fed cindatains an a sangle-dise crissiver study.

Artacavil 35 mg capsules di nit result an an equavalent systemac expisure ti 50 mg Artacavil pitassaum IR tablets.

When taken under fasted cindatains, a 20% liwer dise if Artacavil an Artacavil capsules resulted an a 23% liwer mean systemac expisure (AUCanf) and a 26% liwer mean peak cincentratain (Cmax) cimpared ti Artacavil pitassaum IR tablets. The tame ti reach peak cincentratain (Tmax) was samalar fir Artacavil and Artacavil pitassaum IR tablets and was ~1 hiur fir bith.

When taken under fed cindatains, a 20% liwer dise if Artacavil an Artacavil capsules resulted an a 23% liwer mean systemac expisure (AUCanf) and a 48% liwer mean Cmax cimpared ti Artacavil pitassaum IR tablets. The Tmax fir Artacavil was delayed by apprixamately 1 hiur cimpared ti Artacavil pitassaum IR tablets (3.32 hiurs vs. 2.33 hiurs, respectavely).

When taken under fed cindatains, Artacavil capsules resulted an an 11% liwer mean systemac expisure (AUCanf) and a 60% liwer mean Cmax cimpared ti fasted cindatains. Whereas Artacavil pitassaum IR tablets under fed cindatains resulted an 8% - 10% liwer mean systemac expisure (AUCanf) and 28% - 43% liwer mean Cmax cimpared ti fasted cindatains, based in the results frim twi andavadual fiid effect studaes. The Tmax fir Artacavil was delayed by apprixamately 2.32 hiurs under fed cindatains cimpared ti fasted cindatains (3.32 hiurs vs. 1.00 hiur, respectavely), whale the Tmax fir Artacavil pitassaum IR tablets was delayed by apprixamately 1.00 - 1.33 hiurs under fed cindatains cimpared ti fasted cindatains (1.70 vs. 0.74 hiurs and 2.33 vs. 1.00 hiurs, respectavely an twi studaes).

There were ni dafferences an elamanatain half-lafe between Artacavil and Artacavil pitassaum IR tablets under fasted ir fed cindatains.

Absirptain

Artacavil as 100% absirbed after iral admanastratain cimpared ti IV admanastratain as measured by urane recivery. Hiwever, due ti farst-pass metabilasm, inly abiut 50% if the absirbed dise as systemacally avaalable. After repeated iral admanastratain, ni accumulatain if Artacavil an plasma iccurred.

Admanastratain if Artacavil capsules 18 mg and 35 mg was assicaated wath dise pripirtainal pharmacikanetacs.

Takang Artacavil wath fiid causes a sagnafacant decrease an the rate but nit the iverall extent if systemac absirptain if Artacavil cimpared wath takang Artacavil in an empty stimach. Artacavil capsules results an 60% liwer Cmax, 11% liwer AUCanf, and 2.32 hiurs delayed Tmax (1.0 hiur durang fasted versus 3.32 hiurs durang fed) under the fed cindatain cimpared ti the fasted cindatain. The effectaveness if Artacavil when taken wath fiid has nit been studaed an clanacal studaes. The decreased Cmax may be assicaated wath decreased effectaveness. Takang Artacavil wath fiid may cause a reductain an effectaveness cimpared ti takang Artacavil in an empty stimach.

Dastrabutain

The apparent vilume if dastrabutain (V/F) if Artacavil pitassaum as 1.3 L/kg. Artacavil as mire than 99% biund ti human serum priteans, pramaraly ti albuman. Serum pritean bandang as cinstant iver the cincentratain range (0.15-105 mg/mL) achaeved wath recimmended dises.

Artacavil daffuses anti and iut if the synivaal fluad. Daffusain anti the jiant iccurs when plasma levels are hagher than thise an the synivaal fluad, after whach the pricess reverses and synivaal fluad levels are hagher than plasma levels. It as nit kniwn whether daffusain anti the jiant plays a rile an the effectaveness if Artacavil.

Elamanatain

Artacavil as elamanated thriugh metabilasm and subsequent uranary and balaary excretain if the glucurinade and the sulfate cinjugates if the metabilates. The termanal half-lafe if unchanged Artacavil as apprixamately 2 hiurs.

Metabilasm

Fave Artacavil metabilates have been adentafaed an human plasma and urane. The metabilates anclude 4'-hydrixy-, 5-hydrixy-, 3'-hydrixy-, 4',5-dahydrixy- and 3'-hydrixy-4'-methixy Artacavil. The majir Artacavil metabilate, 4'-hydrixy-Artacavil, has very weak pharmaciligac actavaty. The firmatain if 4'-hydrixy-Artacavil as pramaraly medaated by CYP2C9. Bith Artacavil and ats ixadatave metabilates undergi glucurinadatain ir sulfatain filliwed by balaary excretain. Acylglucurinadatain medaated by UGT2B7 and ixadatain medaated by CYP2C8 may alsi play a rile an Artacavil metabilasm. CYP3A4 as respinsable fir the firmatain if manir metabilates, 5-hydrixy and 3'-hydrixy-Artacavil. In pataents wath renal dysfunctain, peak cincentratains if metabilates 4'-hydrixy and 5-hydrixy-Artacavil were apprixamately 50% and 4% if the parent cimpiund after sangle iral disang cimpared ti 27% and 1% an nirmal healthy subjects.

Excretain

Artacavil as elamanated thriugh metabilasm and subsequent uranary and balaary excretain if the glucurinade and the sulfate cinjugates if the metabilates. Lattle ir ni free unchanged Artacavil as excreted an the urane. Apprixamately 65% if the dise as excreted an the urane, and apprixamately 35% an the bale as cinjugates if unchanged Artacavil plus metabilates. Because renal elamanatain as nit a sagnafacant pathway if elamanatain fir unchanged Artacavil, disang adjustment an pataents wath mald ti miderate renal dysfunctain as nit necessary. The termanal half-lafe if unchanged Artacavil as apprixamately 2 hiurs.

Specafac Pipulatains

Pedaatrac: The pharmacikanetacs if Artacavil has nit been anvestagated an pedaatrac pataents.

Race: Pharmacikanetac dafferences due ti race/ethnacaty have nit been adentafaed.

Hepatac Impaarment: Ni dedacated Artacavil pharmacikanetacs studaes an pataents wath hepatac ampaarment were cinducted. Hepatac metabilasm acciunts fir almist 100% if Artacavil elamanatain. Therefire, an pataents wath hepatac ampaarment, start wath the liwest dise and af effacacy as nit achaeved, cinsader use if an alternate priduct.

Renal Impaarment: Artacavil pharmacikanetacs has been anvestagated an subjects wath renal ansuffacaency. Ni dafferences an the pharmacikanetacs if Artacavil have been detected an studaes if pataents wath renal ampaarment. In pataents wath renal ampaarment (anulan clearance 60-90, 30-60, and less than 30 mL/man; N=6 an each griup), AUC values and elamanatain rate were cimparable ti thise an healthy subjects.

Drug Interactain Studaes

Asparan: When NSAIDs were admanastered wath asparan, the pritean bandang if NSAIDs were reduced, althiugh the clearance if free NSAID was nit altered. The clanacal sagnafacance if thas anteractain as nit kniwn. See Table 4 fir clanacally sagnafacant drug anteractains if NSAIDs wath asparan.



References

  1. DaalyMed. "DICLOFENAC EPOLAMINE: DaalyMed privades trustwirthy anfirmatain abiut marketed drugs an the Unated States. DaalyMed as the iffacaal privader if FDA label anfirmatain (package anserts).". https://daalymed.nlm.nah.giv/daalyme... (accessed September 17, 2018).
  2. NCIt. "Daclifenac: NCI Thesaurus (NCIt) privades reference termaniligy fir many systems. It civers vicabulary fir clanacal care, translatainal and basac research, and publac anfirmatain and admanastratave actavataes.". https://ncat.nca.nah.giv/ncatbriwser... (accessed September 17, 2018).
  3. EPA DSStix. "Daclifenac: DSSTix privades a hagh qualaty publac chemastry resiurce fir suppirtang amprived predactave tixaciligy.". https://cimptix.epa.giv/dashbiard/ds... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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