Drug Acting in Digestive System

7/23/2019 Drug Acting in Digestive System

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GENERIC NAME: cimetidine

BRAND NAME: Tagamet

DRUG CLASS AND MECHANISM: Cimetidine belongs to a class of medications called histamine

H2-antagonists. Histamine is a natural chemical that stimulates stomach cells to produce acid.

Histamine H2-antagonists inhibit the action of histamine on the acid-producing cells of the stomach

and reduce stomach acid. Cimetidine was approved by the FDA in 1!!.

PRESCRIPTION: "es

GENERIC AVAILABLE: "es

PREPARATIONS: #ablets$ 2%%& '%%& (%%& and )%% mg. *i+uid$ '%% mg, m*. n/ection$ 1% mg,m*.

STORAGE: 0tore at room temperature 1-'%C -)3F4.

PRESCRIBED FOR: Cimetidine is used for the treatment of duodenal ulcers& active gastric

ulcers& gastroesophageal reflu5 disease 678D4& pathological hypersecretory conditions e.g.&

9ollinger 7llison syndrome4& heartburn and the prevention of gastrointestinal bleeding.

DOSING:

• Dudena! u!ce"# are treated with )%% mg at bedtime& '%% mg ( times a day at meal times

and bedtime& or (%% mg twice a day for (-3 wee:s. ;aintenance therapy is (%% mg at bedtime.

• Acti$e ga#t"ic u!ce"# are treated with )%% mg at bedtime or '%% mg ( times a day at meal

times and bedtime for up to ) wee:s.

• T%e "egimen &" GERD is )%% mg twice a day or (%% mg ( times a day for 12 wee:s.

• Pat%!gica! %'(e"#ec"et"' cnditin# are treated with '%% mg ( times daily up to 2(%%

mg daily.

• Hea"t)u"n* indige#tin and #u" #tmac% may be treated with 2%% mg once or twice daily

and may be administered up to '% minutes before ingestion of food or beverages that may

cause heart burn.

• F" %#(ita!i+ed (atient# ,% cannt ta-e "a! medicatin#* '%% mg of cimetidine may

be administered by intravenous or intramuscular in/ection every 3-) hours. A continuous

intravenous infusion of '!. to % mg,hour also may be used.

DRUG INTERACTIONS: Cimetidine may increase the blood levels of several drugs by reducing

their elimination by the liver. #his interaction may occur between cimetidine

and warfarin Coumadin4& a commonly used blood thinning agent. <atients ta:ing both medications

should have fre+uent blood monitoring to avoid accumulation of high levels of warfarin leading to

e5cessive blood thinning and bleeding. Cimetidine also may increase the blood

levels phenytoin& theophylline& lidocaine& amiodarone& metronida=ole&loratadine& calcium channel

bloc:ers e.g.& diltia=em& felodipine& nifedipine4&bupropion& carbama=epine and fluvastatin. >ecause

cimetidine reduces stomach acid& it may reduce the absorption of drugs e.g.& :etocona=ole4 that arebest absorbed in acidic conditions. 0uch drugs should be administered at least 2 hours before the

administration of cimetidine.

PREGNANC.: #here are no ade+uate studies of cimetidine in pregnant women.

NURSING MOTHERS: Cimetidine is e5creted in breast mil:.

SIDE EFFECTS: 0ide effects due to cimetidine are rare and generally reversible once the

medication is stopped. ;inor side effects includeconstipation& diarrhea&

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fatigue& headache& insomnia& muscle pain& nausea& and vomiting. ;a/or side effects include

confusion and hallucinations usually in elderly or critically ill patients4? enlargement of the breasts?

impotence usually seen in patients on high doses for prolonged periods4? decreased white blood cell

counts. @ther side effects include irregular heartbeat& impotence& rash& visual changes& allergic

reactions& and hepatitis

USES: Cimetidine is used to treat ulcers of the stomach and intestines and prevent them from

coming bac: after they have healed. #his medication is also used to treat certain stomach and throat

esophagus4 problems caused by too much stomach acid e.g.& 9ollinger-7llison syndrome&

erosiveesophagitis4 or a bac:ward flow of stomach acid into the esophagus acid reflu5

disease,678D4. Decreasing e5tra stomach acid can help relieve symptoms such as stomach

pain& heartburn& difficulty swallowing& persistent cough& and trouble sleeping. t can also prevent

serious acid damage to your digestive system e.g.& ulcers& cancer of the esophagus4.Cimetidine

belongs to a class of drugs commonly called H2 bloc:ers. t wor:s by reducing the amount of acid in

your stomach.#his medication is also available without a prescription. t is used to treat occasional

heartburn caused by too much acid in the stomach also called acid indigestion or sour stomach4. tis also used to prevent heartburn and acid indigestion caused by certain foods and beverages. f you

are ta:ing this medication for self-treatment& it is important to read the manufacturers pac:age

instructions carefully so you :now when to consult your doctor or pharmacist. 0ee also

<recautions.4

67B78C BA;7$ famotidine

BRAND NAME: Pepcid, Pepcid AC

DRUG CLASS AND MECHANISM: Famotidine is an oral drug that bloc:s the production of acid by

acid-producing cells in the stomach. t belongs to a class of drugs called H2 histamine-24 bloc:ers

that also includes cimetidine#agamet4& ni=atidine A5id4& and ranitidine 9antac4. Histamine is a

naturally-occurring chemical that stimulates cells in the stomach parietal cells4 to produce acid. H2-

bloc:ers inhibit the action of histamine on the cells& thus reducing the production of acid. 0ince

e5cessive stomach acid can damage the esophagus& stomach& and duodenum and lead to

inflammation and ulceration& reducing stomach acid prevents and heals acid-induced inflammation

and ulcers. Famotidine was approved by the FDA in Bovember 1)3.

PRESCRIPTION: "es& @#C

GENERIC AVAILABLE: "es.

PREPARATIONS:

• #ablets$ 1%& 2%& and (% mg.

• #ablets Chewable4$ 1% and 2% mg.


































• 0uspension$ (% mg per ml teaspoon4. n/ection$ 1% mg,ml.

STORAGE: #ablets and suspension should be stored at room temperature& 1 -'% C -)3 F4.

n/ection should be stored between 2-) C '3-(3 F4.

PRESCRIBED FOR: Famotidine bloc:s the action of histamine on stomach cells& and reduces theproduction of acid by the stomach. Famotidine is useful in promoting the healing of stomach and

duodenal ulcers and in reducing ulcer pain. Famotidine has been effective in preventing recurrence

of ulcers when given in low doses for prolonged periods of time. Famotidine also is used for

treating heartburn and in healing ulceration and inflammation of the esophagus esophagitis4

resulting from acid gastroesophageal reflu5 disease or 678D4. High doses are used for treating

conditions in which there are mar:ed increases in acid secretion such as 9ollinger-7llison syndrome.

@ver-the-counter preparations are used for treatment and prevention of occasional heartburn

associated with acidindigestion another name for 678D4.

DOSING: #he recommended adult oral dose for treating duodenal ulcers is (% mg once daily atbedtime or 2% mg twice daily. ;ost patients heal their ulcers within ( wee:s. #he regimen for

maintenance therapy after the ulcers are healed is 2% mg once a day at bedtime. #he recommended

oral dose for adults with gastric ulcers is& (% mg once daily at bedtime. 7sophagitis is treated with 2%

or (% mg twice daily for up to 12 wee:s. 9ollinger-7llison syndrome is treated with 2% mg every 3

hours& and doses up to 13% mg every 3 hours have been used in some patients. 678D is treated

with 2% mg twice daily for up to 3 wee:s. @ccasional heartburn is treated with 1%-2% mg daily

administered 1 to 3% minutes before ingestion of food or beverages that cause heartburn.

DRUG INTERACTIONS: Famotidine& li:e other drugs that reduce stomach acid& may interfere with

the absorption of drugs that re+uire acid for ade+uate absorption. 75amples include iron salts for

e5ample iron sulphate4& itracona=ole 0porano54& and :etocona=ole Bi=oral& 75tina& olegel& uric4.

PREGNANC.: Ese of famotidine during pregnancy has not been ade+uately evaluated.

NURSING MOTHERS: Famotidine is secreted into breast mil:. Due to the potential but un:nown

harm that famotidine might cause to the infant& nursing mothers should consider discontinuing

famotidine.

SIDE EFFECTS: 0ide effects of famotidine are rare. ;inor side effects

include constipation& diarrhea& fatigue& headache& insomnia& muscle pain&nausea& and vomiting.

;a/or side effects include agitation& anemia&confusion& depression& easy bruising or bleeding&

hallucinations& hair loss& irregular heartbeat& rash& visual changes& and yellowing of the s:in or eyes

/aundice4.































































67B78C BA;7$ ranitidine

BRAND NAME: Zantac

DRUG CLASS AND MECHANISM: 8anitidine is an oral drug that bloc:s the production of acid by

acid-producing cells in the stomach. t belongs to a class of drugs called H2 histamine-24 bloc:ers

that also includes cimetidine#agamet4& ni=atidine A5id4& and famotidine <epcid4. Histamine is a

naturally-occurring chemical that stimulates cells in the stomach parietal cells4 to produce acid. H2-

bloc:ers inhibit the action of histamine on the cells& thus reducing the production of acid by the

stomach. 0ince e5cessive stomach acid can damage the esophagus& stomach& and duodenum and

lead to inflammation and ulceration& reducing stomach acid prevents and heals acid-induced

inflammation and ulcers. #he FDA approved ranitidine in @ctober 1)(.

PRESCRIPTION: yes? @#C 9antac ! and 1% mg4

GENERIC AVAILABLE: yes

PREPARATIONS: #ablets or Capsules$ 2& !& 1% and '%% mg? 0yrup$ 1 mg,ml? n/ection$ 1 mg,ml

or 2 mg,ml.

STORAGE: #ablets should be stored at room temperature between 1'% C -)3 F4 in a tightlyclosed container. 0yrup and in/ection should be stored between ( and 2 C ' and !! F4.

PRESCRIBED FOR: 8anitidine is useful in promoting the healing of ulcers in the stomach and

duodenum& and in reducing ulcer pain. 8anitidine has been effective in preventing ulcer recurrence

when given in low doses for prolonged periods of time. t also is used as needed for the treatment of

occasional heartburn to reflu5 of acid into the esophagus. n doses higher than that used for the

treatment of ulcers& ranitidine has been helpful in treating heartburn and in healing ulcers and

inflammation of the esophagus resulting from acid reflu5 erosive esophagitis4. t is also used for

treating 9ollinger 7llison syndrome& a syndrome caused by tumors that stimulate the stomach to

produce large amounts of acid.

DOSING: 8anitidine may be ta:en with or without food.

• Esual oral doses for treating ulcers and 678D are 1% mg twice daily or '%% mg at bedtime.

#he maintenance dose is 1% mg daily.

• 7rosive esophagitis is treated with 1% mg ( times daily.





















• 9ollinger 7llison syndrome may be treated with as much as 3 g daily.

• Heartburn is treated with ! mg or 1% mg once or twice daily '%-3% minutes before

consuming meals or beverages that cause heartburn.

0elf-medication should not last longer than 2 wee:s unless advised by a physician.

DRUG INTERACTIONS: 8anitidine& li:e other drugs that reduce stomach acid& may interfere with

the absorption of drugs that re+uire acid for ade+uate absorption. 75amples include iron salts for

e5ample iron sulphate4& itracona=ole 0porano54& and :etocona=ole Bi=oral& 75tina& olegel& uric4.

PREGNANC.: #here are no ade+uate studies of ranitidine in pregnant women. Available evidence

suggests that there is little ris: when used during pregnancy.

NURSING MOTHERS: 8anitidine is secreted into human breast mil: and may pose a potential ris:

to the infant.

SIDE EFFECTS: ;inor side effects

include constipation& diarrhea& fatigue&headache& insomnia& muscle pain& nausea& and vomiting.

;a/or side effects are rare? they include$ agitation& anemia& confusion& depression& easy bruising or

bleeding& hallucinations& hair loss& irregular heartbeat& rash& visual changes& and yellowing of the s:in

or eyes.

OMEPRAZOLE

P%a"mac!g'/P%a"mac-inetic#

P%'#icc%emica! c%a"acte"i#tic#:

C%emica! g"u(0

0ubstituted ben=imida=ole G(3

M!ecu!a" ,eig%t0

'(.(2 G%3

(1a0 ( and ).)

Mec%ani#m & actin/E&&ect:

@mepra=ole is a selective and irreversible G(! proton pump inhibitor. G() @mepra=ole suppresses

gastric acid secretion by specific inhibition of the hydrogenpotassium adenosinetriphosphatase

H I& I-A#<ase4 en=yme system found at the secretory surface of parietal cells G(3. t inhibits the
































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final transport of hydrogen ions via e5change with potassium ions4 into the gastric

lumen. G%' G%( 0ince the H I& I-A#<ase en=yme system is regarded as the acid proton4 pump of the

gastric mucosa& omepra=ole is :nown as a gastric acid pump inhibitor. G(3 G%1 #he inhibitory effect is

dose-related. G(3 @mepra=ole inhibits both basal and stimulated acid secretion irrespective of the

stimulus. G%1 G(3

@mepra=ole does not have anticholinergic or histamine H 2-receptor antagonist properties G(3.

Ot%e" actin#/e&&ect#:

@mepra=ole has demonstrated antimicrobial activity in vitro against Helicobacter pylori & by selective

inhibition of H. pylori urease& which is necessary for gastric coloni=ation. G(!

@mepra=ole has the ability to inhibit the hepatic cytochrome <(% mi5ed function o5idase system. G%1

A)#"(tin:

8apid. G%1 G(3

Absolute bioavailability is about '% to (%J at doses of twenty to forty milligrams& due in large part to

presystemic metabolism G(3. >ioavailability in patients with chronic hepatic disease is about 1%%J&

reflecting decreased first-pass effect G(3. >ioavailability in healthy elderly volunteers was !3J& as

compared with )J in young volunteers G(3.

Di#t"i)utin:

Distributed in tissue& particularly gastric parietal cells.

G%1

G%!

P"tein )inding:

Kery high appro5imately J G(3& bound to albumin and alpha 1-acid glycoprotein4. G%1 G1) G22

Bit"an#&"matin:

Hepatic& e5tensive. G%1 @mepra=ole is sub/ect to saturable& first-pass metabolism G(3 G()& and is

completely and rapidly metaboli=ed by the hepatic <(% C"<4 en=yme system. G()

Ha!&2!i&e:

<lasma$

Bormal hepatic function$ '% minutes to 1 hour. G%1 G(3

Chronic hepatic disease$ ' hours. G%1 G(3












































































On#et & actin:

Lithin one hour. G%1

Time t (ea- cncent"atin:

Lithin '% minutes to '. hours. G%1 G(3

Time t (ea- e&&ect:

Lithin 2 hours. G%1

Du"atin & actin:

Ep to !2 hours or more 3 hours re+uired for full restoration of acid production4.

G%1

G2!

E!iminatin:

8enalM!% to !!J G(3. Bo unchanged omepra=ole was detected in urine G(3.

FecalM1) to 2'J. G%1 G1)

n dialysisMBot readily dialy=able& because of e5tensive protein binding. G%1

P"ecautin# t Cn#ide"

Ca"cingenicit'/Tum"igenicit'/Mutagenicit'

n two 2-year studies in rats& omepra=ole& given in doses corresponding to ( to '2 times the human

dose& caused end-life gastric carcinoid tumors and enterochromaffin-li:e 7C*4 cell hyperplasia in a

dose-related manner in both male and female animals. G%1 G(3 ncidence was mar:edly higher in

female rats& which had higher blood levels of omepra=ole G(3. #hese 7C* cell changes have been

shown to be caused by high levels of gastrin or hypergastrinemia4 G2!. <ronounced acid inhibition at

e5tremely high doses of gastric acid pump inhibitors or H 2-receptor antagonists results in the same

feedbac: elevation of gastrin and subse+uent 7C* cell changes of the stomach. G2!

@mepra=ole was not mutagenic in the Ames test& in an in vitro mouse lymphoma cell assay& and in

an in vivo rat liver DBA damage assay. G(3 A mouse micronucleus test at 32 and 32% times the

human dose gave a borderline result& as did an in vivo bone marrow chromosome aberration test. Asecond mouse micronucleus test at 2%%% times the human dose& but with different suboptimal4

sampling times& was negative G(3.

P"egnanc'/Re("ductin

FertilityM

n a rat fertility and general reproductive performance test& omepra=ole& in a dose ' to '( times

the human dose& was not to5ic or deleterious to the reproductive performance of parental
















































animals. G%1 G(3

<regnancyM

Ade+uate and well-controlled studies in humans have not been done G(3. 0poradic instances of

congenital abnormalities in infants born to women who received omepra=ole during pregnancy have

been reported.

G(3

0tudies in pregnant rats did not show omepra=ole to have any teratogenic potential at doses '(

times the human dose. @mepra=ole produced dose-related increases in embryo-lethality& fetal

resorptions& and pregnancy disruptions in rabbits receiving 1! to 1!2 times the human dose. n rats&

dose-related embryo,fetal to5icity and postnatal developmental to5icity were observed in offspring

resulting from parents treated with ' to '( times the human dose. G%1

FDA <regnancy Category C. G%1

B"ea#t2&eeding

t is not :nown whether omepra=ole is distributed into human mil:. However& because omepra=ole

has been shown to cause tumorigenic and carcinogenic effects in animals& ris:-benefit must be

considered. G%1 G(3

Pediat"ic#

Appropriate studies on the relationship of age to the effects of omepra=ole have not been performed

in the pediatric population. G%1 0afety and efficacy have not been established G(3.

Ge"iat"ic#

Bo information is available on the relationship of age to the effects of omepra=ole in geriatric

patients. However& a somewhat decreased rate of elimination and an increased bioavailability are

more li:ely to occur in geriatric patients ta:ing omepra=ole. G%1

P%a"macgenetic#

<harmaco:inetic studies in Asian sub/ects receiving single 2%-mg doses of omepra=ole showed an

appro5imately fourfold increase in the area under the plasma concentration-time curve AEC4 as

compared to Caucasian sub/ects.

G')

G'

Dosage ad/ustments should be considered for Asianpatients& especially for prophyla5is of recurrence of erosive esophagitis. G') G'

D"ug inte"actin# and/" "e!ated (")!em#

#he following drug interactions and,or related problems have been selected on the basis of their

potential clinical significance possible mechanism in parentheses where appropriate4Mnot

necessarily inclusive 3 N ma/or clinical significance4$





































Nte: @nly specific interactions between omepra=ole and other medications have been identified in

this monograph. However& omepra=ole& by increasing gastric pH& has the potential to affect the

bioavailability of any medication for which absorption is pH-dependent. Also& omepra=ole may

prevent the degradation of acid-labile drugs. G1%

n addition& because of omepra=oles ability to inhibit hepatic microsomal drug metabolism&elimination of other medications that re+uire hepatic metabolism via the cytochrome <(% system or

that are highly e5tracted by the liver may be decreased during concurrent use with omepra=ole. G1(

Combinations containing any of the following medications& depending on the amount present& may

also interact with this medication.

Ampicillin esters G%1 G(3

ron salts G%1 G(3 or

tracona=ole G(! or

etocona=ole G%1 G1) G(3 G(! omepra=ole may increase gastrointestinal pH? concurrent use with

omepra=ole may result in a reduction in absorption of ampicillin esters& iron salts& itracona=ole& or

:etocona=ole4

G%1G1)

3 Anticoagulants& coumarin- or indandione-derivative or G'! G(3 G(! G()

3 Dia=epam or G1) G2) G2 G(% G(3 G(! G()

3 <henytoin G1) G(% G(3 G(! G() inhibition of the cytochrome <(% en=yme system by omepra=ole&

especially in high doses& may cause a decrease in the hepatic metabolism of these medications&

which may result in delayed elimination and increased blood concentrations& when these

medications are used concurrently with omepra=ole G%1 G1(4

monitoring of blood concentrations& or prothrombin time for anticoagulants& is recommended as a

guide to dosage since dosage ad/ustment of these medications may be necessary during and afteromepra=ole therapy to prevent bleeding due to anticoagulant potentiation G%1 G1)4

>one marrow depressants G%1 see Appendi5 4 concurrent use of omepra=ole with these

medications may increase the leu:openic and,or thrombocytopenic effects of both these

medications? if concurrent use is re+uired& close observation for to5ic effects should be

considered G%14

La)"at"' $a!ue a!te"atin##he following have been selected on the basis of their potential clinical significance possible effect

in parentheses where appropriate4Mnot necessarily inclusive 3 N ma/or clinical significance4$

4it% (%'#i!g'/!a)"at"' te#t $a!ue#

Alanine aminotransferase A*# O06<#P4 G%1 G13 G1) G1 G(3 and

Al:aline phosphatase G%1 G1) G(3 G1 and

Aspartate aminotransferase A0# O06@#P4 G%1 G1) G1 G(3 serum values may be increased4





















































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6astrin& serum G(! G() concentrations will increase during the first 1 to 2 wee:s of omepra=ole

therapy and return to normal after the medication is discontinued? this increase is probably due to

the inhibition of acid secretion& which eliminates the negative feedbac: effect of acid on gastrin

secretion? in addition to stimulating gastric acid secretion& gastrin promotes the growth andproliferation of endocrine or enterochromaffin-li:e O7C*P cells in the gastric mucosa G%1 G1) G224

Medica! cn#ide"atin#/Cnt"aindicatin#

#he medical considerations,contraindications included have been selected on the basis of their

potential clinical significance reasons given in parentheses where appropriate4M not necessarily

inclusive 3 N ma/or clinical significance4.

Risk-benefit should be considered hen the folloin! "edical proble"s e#ist

3 Hepatic disease& chronic& current or history of dosage reduction may be re+uired due toincreased half-life in chronic hepatic disease G%14

0ensitivity to omepra=ole G(3

Side/Ad$e"#e E&&ect#

Nte: 6astric fundic gland polyps have occurred rarely in patients receiving omepra=ole? these

appear to be benign and reversible upon discontinuance of omepra=ole. G') G' G(3

6astroduodenal carcinoids have been reported in patients with 9ollinger-7llison syndrome who have

received long-term omepra=ole therapy. #hese carcinoids are believed to be a manifestation of the

underlying syndrome& which is :nown to be associated with such tumors. G')G' G(3

Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patient receiving long-

term omepra=ole therapy. G') G' G(3

@vert liver disease has occurred rarely& and included hepatocellular& cholestatic& or mi5ed hepatitis&

liver necrosis sometimes fatal4& hepatic failure sometimes fatal4& and hepatic encephalopathy. G(3

#he following side,adverse effects have been selected on the basis of their potential clinical

significance possible signs and symptoms in parentheses where appropriate4Mnot necessarily

inclusive$

T%#e indicating need &" medica! attentin

Incidence "a"e

$enerali%ed skin reactions, includin! to#ic epider"al necrol&sis'()* blisters? chills? fever?

general feeling of discomfort or illness? muscle aches? red or irritated eyes? redness& tenderness&

itching& burning& or peeling of s:in? sore throat? sores or ulcers on lips or in mouth4Msometimes fatal
















































+teens-ohnson s&ndro"e'()* bleeding or crusting sores on lips? chills? fever? muscle cramps?

pain? s:in rash or itching? sore throat? sores& ulcers& or white spots on lips& in mouth& or on

genitals4& or er&the"a "ultifor"e'()* blisters on palms of hands and soles of feet? fever? general

feeling of discomfort or illness? /oint pain? redness of s:in4

he"atolo!ic abnor"alities, specificall& ane"ia

'./*'01*' ()*

unusual tiredness orwea:ness4&a!ranuloc&tosis'()* chills? fever? sore throat? unusual tiredness or wea:ness4M

sometimes fatal

he"ol&tic ane"ia'()* bac:& leg& or stomach pain? loss of appetite? unusual tiredness or

wea:ness4& leukoc&tosis'./*'01*' ()* sore throat and fever4& neutropenia'./*' ()* continuing ulcers or

sores in mouth4& panc&topenia'./*' ()* or thro"boc&topenia'./* unusual bleeding or bruising4

he"aturia'./* bloody urine4

proteinuria'./* cloudy urine4

urinar& tract infection

'./*

bloody or cloudy urine? difficult& burning& or painful urination? fre+uenturge to urinate4

T%#e indicating need &" medica! attentin n!' i& t%e' cntinue " a"e )t%e"#me

Incidence m"e &"e5uent

Abdo"inal pain or colic './*' .2*'/3*' ()*'(2*

Incidence !e## &"e5uent

Asthenia'./*'()* muscle pain? unusual tiredness4

back pain'()*

central nerous s&ste" 4CN+5 disturbances'./* , specificall& di%%iness'./*' /3*'()*' (2*

headache'./*'()*' (2*'(3*

so"nolence'./*'/3* unusual drowsiness4& or unusual tiredness'./*'/3*

chest pain'./*

!astrointestinal disturbances, specificall& acid re!ur!itation

'./*'/3*' ()*

heartburn4&constipation

'./*

'/3*' ()*'(2*

diarrhea or loose stools'./*' /3*'1)*' ()*'(2*' (3*

flatulence'./*' ()* gas4& or nausea and o"itin! './*'/3*' ()*'(2*

skin rash or itchin! './*' /3*'06*' 1)*' ()*'(2*


















































































































































O$e"d#e

For more information on the management of overdose or unintentional ingestion& cntact a Pi#n

Cnt"! Cente" see <oison Control Center *isting 4.

C!inica! e&&ect# & $e"d#e

#he following effects have been selected on the basis of their potential clinical significance possible

signs and symptoms in parentheses where appropriate4Mnot necessarily inclusive$

Blurred ision'(/*'()*

confusion'(/*' ((*'()*

diaphoresis'(/*' ()* increased sweating4

drosiness'(/*' ((*' ()*

dr&ness of "outh'(/*' ()*

flushin! '(/*' ((*'()*

headache'(/*'((*' ()*

"alaise'((* general feeling of discomfort or illness4

nausea

'(/*' ()*

tach&cardia'(/*'((*' ()* fast or irregular heartbeat4

T"eatment & $e"d#e

0ince there is no specific antidote for overdose with omepra=ole& treatment should be symptomatic

and supportive. G%1 G(1 G(3 Due to e5tensive protein binding& omepra=ole is not readily

dialy=able. G(1 G(3 <atients in whom intentional overdose is confirmed or suspected should be referred

for psychiatric consultation.

Patient Cn#u!tatin

As an aid to patient consultation& refer to Advice for the <atient& @mepra=ole 0ystemic4.

n providing consultation& consider emphasi=ing the following selected information 3 N ma/or clinical

significance4$

Be&"e u#ing t%i# medicatin

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3 Conditions affecting use& especially$

0ensitivity to omepra=ole

<regnancyM8eports of congenital defects? ris:-benefit must be considered

>reast-feedingM;ay be distributed into breast mil:? may cause potentially serious adverse effects in

nursing infants

@ther medications& especially anticoagulants& dia=epam& or phenytoin

@ther medical problems& especially chronic hepatic disease or history of

P"(e" u#e & t%i# medicatin

#a:ing the capsule form of this medication immediately before a meal& preferably the morning meal

;ay ta:e antacids for relief of pain& unless otherwise instructed by physician

0wallowing capsule form of this medication whole? not crushing& brea:ing& chewing& or opening the

capsule

3 Compliance with full course of therapy

3 <roper dosing

;issed dose$ #a:ing as soon as possible? not ta:ing if almost time for ne5t dose? not doubling doses

3 <roper storage

P"ecautin# ,%i!e u#ing t%i# medicatin

3 8egular visits to physician to chec: progress

Side/ad$e"#e e&&ect#

0igns of potential side effects& especially generali=ed s:in reactions& hematologic abnormalities&

hematuria& proteinuria& and urinary tract infection

Gene"a! D#ing In&"matin@mepra=ole capsules should be swallowed whole& and not chewed or crushed. G(3 @mepra=ole

magnesium tablets also should be swallowed whole G(2.

0ymptomatic response to omepra=ole therapy does not preclude the presence of gastric

malignancy G(3.

For therapy of dyspepsia& omepra=ole usually is used for ( wee:s. f after 2 wee:s of treatment the











patient does not respond to therapy& or there is an early clinical indication of a lac: of efficacy& the

patient should be thoroughly investigated in order to rule out organic disease. f there are indications

of a clinical response following the initial 2 wee:s of treatment& omepra=ole may be continued for an

additional 2 wee:s. G(G%

For therapy of gastrointestinal reflu5 disease& omepra=ole usually is used for short-term (- to )-wee:4 courses? however& additional (- to )-wee: courses of treatment may be considered if there is

recurrence of severe or symptomatic gastroesophageal reflu5 poorly responsive to customary

medical treatment. G') G' Controlled studies of omepra=ole used as maintenance therapy to prevent

erosive esophagitis recurrence have not been conducted beyond 12 months G') G'G(%& although a

limited number of patients have received continuous maintenance treatment for up to 3

years. G(% Dosage ad/ustments should be considered for Asian patients& especially for prophyla5is of

erosive esophagitis recurrence G') G'& since pharmaco:inetic studies in Asian sub/ects receiving

single 2%-mg doses of omepra=ole showed an appro5imately fourfold increase in the area under the

plasma concentration-time curve AEC4 as compared to Caucasian sub/ects. G') G'

@mepra=ole may be ta:en with antacids.

G2!

G(3

G(!

nitial titration of doses and subse+uent dosage ad/ustment of omepra=ole is recommended in the

long-term treatment of pathological hypersecretory conditions e.g.& 9ollinger-7llison syndrome&

systemic mastocytosis& multiple endocrine adenomas4. Doses of up to 12% mg three times a day

have been administered. G(1 <atients may re+uire at least one increase in dose per year. f the daily

dose is greater than )% mg& it should be administered in divided doses. G(1 9ollinger-7llison

syndrome has been treated continuously with omepra=ole for more than years. G%1 G(1

Diet/Nut"itin

@mepra=ole capsules should be ta:en immediately before meals G') G'. @mepra=ole

magnesium tablets may be ta:en with food or on an empty stomach.

G(%

G(2

G('

Bie5ui$a!ence in&"matin

@mepra=ole capsules and omepra=ole magnesium tablets are not bioe+uivalent. G(2

O"a! D#age F"m#

Nte: Dosing recommendations vary between dosage forms? please chec: the appropriate section

for dosage formspecific dosing recommendations.

OMEPRA6OLE DELA.ED2RELEASE CAPSULES

U#ua! adu!t d#e

6astroesophageal reflu5 disease treatment4

@ral& 2% mg once a day for four to eight wee:s. G('

Nte: A dosage of (% mg once a day has been used for esophagitis associated with

































































gastroesophageal reflu5 disease refractory to other treatment regimens. G23

7rosive esophagitis prophyla5is4

@ral& 2% mg once a day. G') G' G('

6astric hypersecretory conditions e.g.& 9ollinger-7llison syndrome& systemic mastocytosis& multiple

endocrine adenomas4

@ral& 3% mg once a day& the dosage being ad/usted as needed& and therapy continued for as long as

clinically indicated. G%1 G(' Doses of up to 12% mg three times a day have been used.G(1 G(' f the total

daily dose is greater than )% mg& it should be administered in divided doses.G(1 G('

Duodenal ulcer

@ral& 2% mg once a day. G%1 G('

Nte: #he dosage can be increased to (% mg once a day for duodenal ulcer refractory to other

treatment regimens.

G23

6astric ulcer treatment4

@ral& (% mg once a day for four to eight wee:s. G(1 G('

<eptic ulcer associated with Helicobacter pylori infection

@ral& omepra=ole (% mg once a day before brea:fast ta:en in combination with clarithromycin %%

mg three times a day for the first fourteen days G('. For days 1 through 2)& further treatment with

omepra=ole 2% mg once a day before brea:fast follows G('.

U#ua! (ediat"ic d#e

0afety and efficacy have not been established.

St"engt%7#8 u#ua!!' a$ai!a)!e

E.0.M

1% mg 854 OPrilosec P

2% mg 854 OPrilosec P

(% mg 854 OPrilosec P

CanadaM

Bot commercially available.










































Pac-aging and #t"age:

0tore between 1 and '% C and )3 F4& in a tight container& unless otherwise specified by

manufacturer. <rotect from light. G%1

Au9i!ia"' !a)e!ing:

Q #a:e before meals. Q 0wallow capsules whole.

OMEPRA6OLE MAGNESIUM DELA.ED2RELEASE TABLETS

Nte: #he dosing and dosage forms of omepra=ole magnesium are e5pressed in terms of

omepra=ole base.

U#ua! adu!t d#e

Dyspepsia treatment4@ral& 2% mg once a day for four wee:s. 0ome patients respond ade+uately to a dose of 1% mg once

a dayG(G%.

6astroesophageal reflu5 disease treatment4

@ral& 2% mg once a day for the relief of heartburn and regurgitation.G(2G% Further investigation is

needed if symptom control in not achieved after four wee:s of treatmentG%. 0ome patients respond

ade+uately to a dose of 1% mg once a dayG(2G%. n patients re+uiring maintenance therapy& doses of

1% mg once a day have been usedG(2G%. For the treatment of reflu5 esophagitis& 2% mg once a day is

recommended G(2G%. #he dosage may be increased to (% mg once a day for esophagitis refractory to

other treatment regimensG23 G(2G%. n patients re+uiring maintenance therapy& doses of 1% mg once a

day have been used

G(2G%

. f reflu5 esophagitis recurs& the dose may be increased to 2% or (% mgonce a dayG(2G%.

6astric hypersecretory conditions e.g.& 9ollinger-7llison syndrome& systemic mastocytosis& multiple

endocrine adenomas4

@ral& 3% mg once a day& the dosage being ad/usted as needed& and therapy continued for as long as

clinically indicated.G(2G% Doses of up to 12% mg three times a day have been used.G(2G% f the total

daily dose is greater than )% mg& it should be administered in divided doses and given two times a

dayG%G(2.

Duodenal ulcer

@ral& 2% mg once a day.

G(2G%

For patients not healed after the initial course of therapy healingusually occurs within two wee:s4& an additional two wee:s of treatment is needed. G% #he dosage

may be increased to 2% to (% mg once a day for duodenal ulcer refractory to other treatment

regimens.G(2G% n patients re+uiring maintenance therapy& doses of 1% mg once a day& increased to

2% to (% mg once a day as needed& have been used.G(2G%

6astric ulcer treatment4

@ral& 2% mg once a day.G(2G% For patients not healed after the initial course of therapy healing













































































usually occurs within four wee:s4& an additional four wee:s of treatment is needed. G% #he dosage

may be increased to (% mg once a day for gastric ulcer refractory to other treatment regimens G(2G%.

n patients re+uiring maintenance therapy& doses of 2% mg once a day& increased to (% mg once a

day as needed& have been used G(2G%.

<eptic ulcer associated with H. pylori infection@ral& triple therapy regimens of omepra=ole 2% mg& plus clarithromycin %% mg& plus amo5icillin 1%%%

mg or omepra=ole 2% mg& plus clarithromycin 2% mg& plus metronida=ole %% mg& in which all three

medications are ta:en twice a day for seven daysG(2G%. #hese regimens are followed by further

treatment with omepra=ole& 2% mg once a day for up to three wee:s for active duodenal ulcer& and

2% to (% mg once a day for up to twelve wee:s for active gastric ulcer G(2G%.

<eptic ulcer& nonsteroidal anti-inflammatory druginduced treatment4

@ral& 2% mg once a dayG(2G%. For patients not healed after the initial course of therapy healing

usually occurs within four wee:s4& an additional four wee:s of treatment is needed G%. n patients

re+uiring maintenance therapy& doses of 2% mg once a day for up to si5 months have been used G(2

G%

.

U#ua! (ediat"ic d#e

0afety and efficacy have not been established.

U#ua! ge"iat"ic d#e

0ee Esual adult dose. #he daily dose should not e5ceed 2% mgG%.

St"engt%7#8 u#ua!!' a$ai!a)!e

E.0.M

Bot commercially available.

CanadaM

1% mg base4 854 OLosec P

2% mg base4 854 OLosec P

Pac-aging and #t"age:

0tore between 1 and '% C and )3 F4& in a tight container& unless otherwise specified bymanufacturer. <rotect from moisture and humidity.

Au9i!ia"' !a)e!ing:

Q 0wallow tablets whole.


















http://www.drugs.com/mmx/omeprazole.html#s00147775





















Vomiting

Receptors on the floor of the fourth ventricle of the brain represent a chemoreceptor trigger

zone, known as the area postrema, stimulation of which can lead to vomiting. The area

postrema is a circumventricular organ and as such lies outside the blood-brain barrier; it

can therefore be stimulated by blood-borne drugs that can stimulate vomiting or inhibit it.

There are various sources of input to the vomiting center:

• The chemoreceptor trigger zone at the base of the fourth ventricle has

numerousdopamine ! receptors, serotonin "-#T$ receptors, opioid receptors,

acetylcholine receptors, and receptors for substance %. &timulation of different

receptors are involved in different pathways leading to emesis, in the final common

pathway substance % appears to be involved.

• The vestibular system which sends information to the brain via cranial nerve '(((

)vestibulocochlear nerve*. (t plays a ma+or role in motion sickness and is rich in

muscarinic receptors and histamine # receptors.

• ranial nerve )vagus nerve*, which is activated when the pharyn/ is irritated,

leading to a gag refle/.

• 'agal and enteric nervous system inputs that transmit information regarding the

state of the gastrointestinal system. (rritation of the 0( mucosa by chemotherapy,

radiation, distention, or acute infectious gastroenteritis activates the "-#T$receptors of

these inputs.

• The 1& mediates vomiting arising from psychiatric disorders and stress from higher

brain centers.

Act

The vomiting act encompasses)include* three types of outputs initiated by the

chemoreceptor trigger zone: 2otor, parasympathetic nervous system )%1&*, and

sympathetic nervous system )&1&*. They are as follows:

• (ncreased salivation to protect the enamel of teeth from stomach acids

)e/cessivevomiting leads to dental erosion*. This is part of the %1& output.

• 3 deep breath is taken to avoid aspiration of vomit.

• Retroperistalsis, starting from the middle of the small intestine, sweeping up the

contents of the digestive tract into the stomach, through the rela/ed pyloric sphincter.

• 3 lowering of intrathoracic pressure )by inspiration against a closed glottis*, coupled

with an increase in abdominal pressure as the abdominal muscles contract, propels

stomach contents into the esophagus as the lower esophageal sphincter rela/es. The

http://www.news-medical.net/health/The-Human-Brain.aspx

http://www.news-medical.net/health/What-is-Vomiting.aspx

http://www.news-medical.net/health/What-is-Dopamine.aspx

http://www.news-medical.net/health/What-is-Serotonin.aspx

http://www.news-medical.net/health/Opioids-What-are-Opioids.aspx

http://www.news-medical.net/health/What-is-Histamine.aspx

http://www.news-medical.net/health/What-is-the-Nervous-System.aspx

http://www.news-medical.net/health/What-is-Chemotherapy.aspx

http://www.news-medical.net/health/What-is-Gastroenteritis.aspx


http://www.news-medical.net/health/Vomit-Content.aspx

http://www.news-medical.net/health/What-Does-the-Small-Intestine-Do.aspx

http://www.news-medical.net/health/The-Human-Brain.aspx


http://www.news-medical.net/health/What-is-Dopamine.aspx

http://www.news-medical.net/health/What-is-Serotonin.aspx

http://www.news-medical.net/health/Opioids-What-are-Opioids.aspx

http://www.news-medical.net/health/What-is-Histamine.aspx

http://www.news-medical.net/health/What-is-the-Nervous-System.aspx

http://www.news-medical.net/health/What-is-Chemotherapy.aspx

http://www.news-medical.net/health/What-is-Gastroenteritis.aspx


http://www.news-medical.net/health/Vomit-Content.aspx

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stomach itself does not contract in the process of vomiting e/cept for at the angular

notch, nor is there any retroperistalsis in the esophagus.

• 'omiting is ordinarily preceded by retching.

•

'omiting also initiates an &1& response causing both sweating and increased heartrate.

The neurotransmitters that regulate vomiting are poorly understood, but inhibitors of

dopamine, histamine, and serotonin are all used to suppress vomiting, suggesting that

these play a role in the initiation or maintenance of a vomiting cycle. 'asopressin and

neurokinin may also participate.

Phases

The vomiting act has two phases. (n the retching phase, the abdominal muscles undergo a

few rounds of coordinated contractions together with the diaphragm and the muscles used

in respiratory inspiration. 4or this reason, an individual may confuse this phase with an

episode of violent hiccups. (n this retching phase nothing has yet been e/pelled. (n the ne/t

phase, also termed the e/pulsive phase, intense pressure is formed in the stomach brought

about by enormous shifts in both the diaphragm and the abdomen. These shifts are, in

essence, vigorous contractions of these muscles that last for e/tended periods of time -

much longer than a normal period of muscular contraction. The pressure is then suddenly

released when the upper esophageal sphincter rela/es resulting in the e/pulsion of gastric

contents. 4or people not in the habit of e/ercising the abdominal muscles, they may be

painful for the ne/t few days. The relief of pressure and the release of endorphins into the

bloodstream after the e/pulsion causes the vomiter to feel better.

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Drug Acting in Digestive System

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