Pharmacology - Git Drugs

Pharmacology of the GT
system
2005
TUR Outline
R' the Anatomy of the GT
R' the Physiology of the GT
Review common G drugs in the following
categories:
1. Drugs affecting GI secretions
2. Laxatives
3. Anti-diarrheaIs
4. Emetics and anti-emetics
ig. 16.1
ig. 16.10a
ig. 16.10b
ig. 16.11a
ig. 16.11b
ig. 16.12
rugs affecting G secretions
%here are five types of drugs that affect gastric
acid secretions and are usefuI for the
treatment of peptic uIcer.
1. Histamine (H2) receptor antagonist/bIockers
2. Antacids
3. Proton pump inhibitors
4. MucosaI protectants
5. ProstagIandin anaIogs
rugs affecting secretions:
anti ulcer
Anti-ulcer drugs Prototype
Histamine (H2) receptor
antagonist/bIockers
imetidine
Antacids
AlOH and MgOH
Proton pump inhibitors
Omeprazole
MucosaI protectants
Sucralfate
ProstagIandin anaIog
Misoprostol
General indication of the drugs
affecting gastric acid secretion
Peptic ulcer
Gastritis
Patient on NPO to prevent stress ulcer
General time of administration of the
drugs affecting gastric acid secretion
Anti-uIcer drugs Prototype Best time to give
Histamine (H2)
receptor
antagonist/bIockers
Cimetidine With FOOD or ONE
hour after AN%ACID
Antacids
AIOH and MgOH UsuaIIy after meaIs
Proton pump
inhibitors
OmeprazoIe BEFORE MEALS
MucosaI
protectants
SucraIfate BEFORE MEALS
ProstagIandin
anaIog
MisoprostoI WI%H MEALS
Pharmacodynamics
Histamine (H2) receptor bIockers
%hese drugs BLOCK the reIease of
hydrochIoric acid in the stomach in
response to gastrin
Antacids
%hese drugs interact with the
gastric acids at the chemicaI
IeveI to neutraIize them
Proton pump inhibitors
%hese drugs suppress the
secretion of hydrochIoric acid
into the Iumen of the stomach
MucosaI protectants
%hese are agents that coat any
injured area in the stomach to
prevent further injury from acid
ProstagIandin anaIogs
%hese are agents that inhibit the
secretion of gastrin and
increase the secretion of mucus
Iining of the stomach, providing
a buffer.
The H2 Blockers- tidines"
Prototype: Cimetidine
1. Ranitidine
2. Famotidine
3. Nizatidine
The H2 Blockers- "tidines
Pharmacodynamics: Drug Action
%he H2 bIockers are antagonists at the
receptors in the parietaI ceIIs of the
stomach.
%he bIockage resuIts to inhibition of the
hormone gastrin.
%here wiII be decreased production of
gastric acid from the parietaI ceIIs.
AIso, the chief ceIIs wiII secrete Iess
pepsinogen.
%herapeutic use of the H2 bIockers
Short-term treatment of active duodenaI
uIcer or benign gastric uIcer
%reatment of hypersecretory conditions Iike
the ZoIIinger-EIIison syndrome
Prevention of stress-induced uIcers and
acute GI bIeeding
%reatment of erosive GERD (refIux disease)
ReIief of Symptoms of heart burn and acid
indigestion
Precautions and Contraindications
Any known aIIergy is a cIear
contraindication to the use of the agents.
Conditions such as pregnancy, Iactation,
renaI dysfunction and hepatic
dysfunction shouId warrant cautious
use.
izatidine can be used in hepatic
dysfunction.
Dynamics- Side effects/adverse effects
GI% diarrhea or constipation
CNS Dizziness, headache, drowsiness,
confusion and haIIucinations
Cardio arrhythmias, HYPO%ENSION
(reIated to H2 receptor bIockage in the
heart)
Cimetidine necomastia and
impotence in males
Drug-drug Interactions
Cimetidine, Famotidine, Ranitidine
are metaboIized in the Iiver- they
can cause sIowing of excretion of
other drugs Ieading to their
increased concentration.
%he H2 BIockers- "tidines"
Drug-drug Interactions
%hese drugs can interact with CIME%IDINE
AnticoaguIants
Phenytoin,
AIcohoI
Antidepressants.
Nursing considerations:
Administer the drug WITH meaIs at
BEDTIME to ensure therapeutic IeveI
One hour after Antacids
Stress the importance of the
continued use for the Iength of time
prescribed
Nursing considerations
Monitor the cardiovascuIar status
especiaIIy if the drugs are given IV
Warn patient of the potentiaI probIems
of increased drug concentration if the
H2 bIockers are used with other drugs
or O%C drugs. Advise consuItation
first!
Provide comfort measures Iike
anaIgesics for headache, assistance
with ambuIation and safety measures
because of confusion
Warn the patients taking cimetidine that
drowsiness may pose a hazard if
driving or operating deIicate machines.
Provide heaIth teaching as to the dose,
frequency, comfort measures to initiate
when side-effects are intoIerabIe
EvaIuate the effectiveness
ReIief of symptoms of uIcer, heart burn
and GERD
The Antacids
%hese are drugs or inorganic chemicaIs
that have been used for years to
neutraIize acid in the stomach
The Antacids
%he foIIowing are the common antacids
that can be bought O%C:
AIuminum saIts (hydroxide)
CaIcium saIts (carbonate)
Magnesium saIts (miIk of magnesia)
Sodium bicarbonate
MagaIdrate (aIuminum and magnesium
combination)
The Antacids
Pharmacodynamics: drug action
%hese agents act to neutraIize the
acidic pH in the stomach.
The do not affect the rate of gastric
acid secretion.
The Antacids
%he administration of antacid may
cause an acid rebound.
NeutraIizing the stomach content to an
aIkaIine IeveI stimuIates gastrin
production to cause an increase in acid
production and return the stomach to
its normaI acidic state.
The Antacids
%herapeutic Indications
Symptomatic reIief of upset stomach
associated with hyperacidity
Hyperacidic conditions Iike peptic
uIcer, gastritis, esophagitis and hiataI
hernia
$pecial use of AMPHOEL (aluminum
hdroxide): to BID phosphate
The Antacids
Precautions of Antacid Use
Known aIIergy is a cIear
contraindication
Caution shouId be instituted if used in
eIectroIyte imbaIances, GI obstruction
and renaI dysfunction.
Sodium bicarbonate is rareIy used
because of potentiaI systemic
absorption metabolic alkalosis!!!
The Antacids
Pharmacokinetics
%hese agents are taken oraIIy and act
IocaIIy in the stomach
The Antacids
Pharmacodynamics: Effects of drugs
1. GI% rebound acidity; aIkaIosis may
occur.
CaIcium saIts may Iead to hpercalcemia
Magnesium saIts can cause DIARRHEA
AIuminum saIts may cause
O$TIPATIO and Hpophosphatemia
by binding with phosphates in the GI%.
2. Fluid retention due to the high sodium
content of the antacids.
The Antacids
Nursing Considerations:
Administer the antacids apart from any
other medications by OE hour before
or TWO hours after- to ensure adequate
absorption of the other medications
%eII the patient to HEW the tabIet
thoroughIy before swaIIowing.
FoIIow it with one gIass of water
ReguIarIy monitor for manifestations of
acid-base imbaIances as weII as
eIectroIyte imbaIances
The Antacids
Nursing Considerations:
Provide comfort measures to aIIeviate
constipation associated with aIuminum and
diarrhea associated with magnesium saIts.
Monitor for the side-effects, effectiveness of
the comfort measures, patient's response to
the medication and the effectiveness of the
heaIth teachings
The Antacids
Nursing Considerations
EvaIuate for effectiveness:
Decreased smptoms of ulcer and
prosis
Decreased Phosphate level (Amphogel)
in patients with chronic renal failure
The PP
%hese are the newer agents for uIcer
treatment
%he "prazoIes"
Prototype: Omeprazole
Lanisoprazole
Esomeprazole
Pantoprazole
The PP
%hey act at specific secretory surface
receptors to prevent the finaI step of
acid production and thus decrease the
IeveI of acid in the stomach.
%he "pump" in the parietaI ceII is the H-
K A%Pase enzyme system on the
secretory surface of the gastric parietaI
ceIIs
The PP
CIinicaI use of the PPIs
Short-term treatment of active
duodenaI uIcers, GERD, erosive
esophagitis and benign gastric uIcer
Long-term- maintenance therapy for
heaIing of erosive disorders.
The PP
Precautions with the use of the PPIs
Known aIIergy is a cIear
contraindication
Caution if patient is pregnant
The PP
Pharmacodynamics: Adverse effects
CNS- dizziness, headache, asthenia
(Ioss of strength), vertigo, insomnia,
apathy
IT- diarrhea, abdominal pain, nausea,
vomiting, dr mouth and tongue
atrophy
Respi- cough, stuffy nose, hoarseness
and epistaxis.
The PP
Administer the drug BEFORE meaIs.
Ensure that patient does not open,
chew or crush the drug.
Provide safety measures if CNS
dysfunction happens.
Arrange for a medicaI foIIow-up if
symptoms are NO% resoIved after 4-8
weeks of therapy.
The PP
Provide heaIth teaching as to drug
name, dosages and frequency, safety
measures to handIe common probIems.
Monitor patient response to the drug,
the effectiveness of the teaching pIan
and the measures to empIoy
The PP
EvaIuate for effectiveness of the drug
HeaIing of peptic uIcer
Decreased symptoms of uIcer
The Mucosal Protectant
SucraIfate (CaraIfate/ IseIpin)
%his is given to protect the eroded
uIcer sites in the GI% from further
damage by acid and digestive enzymes
Sucralfate
Pharmacodynamics: Action of drug
It forms an ulcer-adherent complex at
duodenaI uIcer sites, protecting the
sites against acid, pepsin and biIe.
%his action prevents further breakdown
of proteins in the area and promotes
heaIing.
Sucralfate
CIinicaI use of sucraIfate
Short and Iong term management of
duodenaI uIcer.
NSAIDs induced gastritis
Prevention of stress uIcer
%reatment of oraI and esophageaI
uIcers due to radiation, chemotherapy
or scIerotherapy.
Sucralfate
Precautions on the use of SucraIfate
%his agent shouId NO% be given to any
person with known aIIergy to the drug,
and to those patients with renaI
faiIure/diaIysis because of buiId-up of
aIuminum may occur if used with
aIuminum containing products.
Pharmacodynamics: Side-effects &
adverse reactions
Primaril IT= O$TIPATIO,
occasionall diarrhea, nausea,
indigestion, gastric discomfort, and dr
mouth ma also occur
CNS dizziness, drowsiness, vertigo
Others rash and back pain
Drug-drug interactions
If used with aluminum salts= high risk
of accumulation of aluminum and
toxicit.
If used with phenytoin,
fIuoroquinoIones and peniciIIamines-
decreased IeveIs of these drugs when
taken with sucraIfate
Administer drug O A EMPTY stomach, 1
hour before meals , or 2 hour after meals and
at BEDTIME
Monitor for side-effects Iike constipation and
GI upset
Encourage intake of high-fiber foods and
increased fIuid intake
Administer antacids BETWEE doses of
sucraIfate, OT WITHI 30 minutes of
sucraIfate dose
Provide comfort measures if CNS
effects occur
Provide heaIth teaching as to drug
name, dosages and frequency, safety
measures to handIe common probIems.
Monitor patient response to the drug,
the effectiveness of the teaching pIan
and the measures empIoyed
EvaIuate effectiveness of therapy
HeaIing of uIcer
No formation of uIcer
Prostaglandin analogue
MisoprostoI
%his agent is a synthetic prostagIandin
E1 anaIog that is empIoyed to protect
the Iining of the mucosa of the stomach
MisoprostoI: Pharmacodynamics
Being a prostagIandin anaIog, it
inhibits gastric acid secretion to some
degree
It IREA$E$ mucus production in the
stomach Iining.
MisoprostoI: CIinicaI use
NSAIDs-induced gastric uIcers
DuodenaI uIcers unresponsive to H2
antagonists
Precautions of MisoprostoI Use
%his drug is CON%RAINDICA%ED during
pregnancy because it is an abortifacient.
Women shouId be advised to have a negative negative
pregnanc test within 2 weeks of beginning pregnanc test within 2 weeks of beginning
therap and should begin the drug on the therap and should begin the drug on the
second or third da of the next menstrual second or third da of the next menstrual
ccle. ccle.
%hey shouId be instructed in the use of
contraceptives during therapy.
Pharmacodynamic effects: drug
reactions
GI% Nausea, diarrhea, abdominaI pain,
fIatuIence, vomiting, dyspepsia
GU effects miscarriages, excessive
uterine RAMPI and bleeding,
spotting, hyper-menorrhea and
menstruaI disorders.
Administer to patients at risk for NSAIDs-
induced uIcers during the fuII course of
NSAIDs therapy
Administer four times daiIy with meaIs and at
bedtime
Obtain pregnancy test within 2 weeks of
beginning therapy.
Begin the therapy on second or third day of
menstruaI period to ensure that the woman is
not pregnant
Provide patient with both written and oraI
information regarding the associated risks of
pregnancy
Provide heaIth teaching as to drug name,
dosages and frequency, safety measures to
handIe common probIems.
Monitor patient response to the drug, the
effectiveness of the teaching pIan and the
measures to empIoy
axatives
GeneraIIy used to INCREASE the
passage of the coIonic contents
%he generaI cIassifications is as
foIIows:
1. ChemicaI stimuIants- irritants
2. MechanicaI stimuIants- hyperosmotic
agents and saIine cathartics
3. Lubricants and stooI softeners
axatives
%hey promote boweI evacuation for
various purposes
%hey are cIassified into their mode of
action
axatives
%ype Prototype Action
ChemicaI
stimuIants
BisacodyI
(DuIcoIax)
Direct stimuIation of the
GI% nerves
Irritant Iaxatives
MechanicaI
(buIk)
stimuIants
LactuIose
Increased fIuid content
of the fecaI materiaI
causing stimuIation of
the IocaI refIex
Lubricants Docusate
MineraI oiI
Lubricating the
intestinaI materiaI to
promote passage
through the GI%
Therapeutic ndications of the
axatives
SHOR% term reIief of onstipation onstipation
Prevention of straining Prevention of straining in conditions
Iike CHF, post-MI, post partum, post-op
Preparation for diagnostic examination diagnostic examination
RemovaI of poison or toxins
Adjunct in anti-heIminthic therapy
%o remove AMMONIA by use of
IactuIose
ontraindications in axative use
ACU%E abdominaI disorders
Appendicitis Appendicitis
Diverticulitis Diverticulitis
Ulcerative colitis Ulcerative colitis
hemical Stimulant athartics
Prototype: BisacodyI
Irritant Iaxatives:
1. Castor oiI
2. Senna
3. Cascara
4. PhenoIphthaIein
hemical Stimulant athartics
Pharmacodynamics
%hese agents DIREC%LY stimuIate the
nerve pIexus in the intestinaI waII
%he resuIt is INCREASED movement or
motiIity of the coIon
Mechanical Stimulant athartics
Prototype: LAC%ULOSE (CephuIac)
BuIk-forming Iaxatives
1. Magnesium (citrate, hydroxide,
suIfate)- saIine cathatic
2. PsyIIium
3. PoIycarbophiI
Mechanical Stimulant athartics
Pharmacodynamics
%hese agents are rapid-acting Iaxatives
that INCREASE the GI motiIity by
Increasing the fIuids in the coIonic
materiaI
StimuIating the IocaI stretch receptors
Activating IocaI defection refIex
ubricants-Stool softener
Prototype: Docusate
1. GIycerin
2. MineraI oiI
ubricants-stool softeners
Pharmacodynamics
Docusate increases the admixture of fat
and water producing a softer stooI
GIycerin and MineraI oiI form a slipper
coat on the colonic contents
Pharmacokinetics:
Common Side-effects of the Laxatives
Diarrhea
AbdominaI cramping
Nausea
FIuid and eIectroIyte imbaIance
Sympathetic reactions- sweating,
paIpitations, fIushing and fainting
CA%HAR%IC dependence
The Nursing Process and axative
ASSESSMEN%
Nursing History- eIicit aIIergy to any
Iaxatives, eIicit history of conditions
Iike diverticuIitis and uIcerative coIitis
PhysicaI Examination- abdominaI
assessment
Laboratory %est: fecaIysis, eIectroIyte
IeveIs
NURSING DIAGNOSIS
AIteration in boweI pattern
AIteration in comfort: pain
KnowIedge deficit
IMPLEMEN%A%ION
1. Emphasize that it is use on a SHOR%
term basis
2. Provide comfort and safety measures
Iike ready access to the bathroom,
side-raiIs
3. Administer with a full glass of water
IMPLEMEN%A%ION
4. Encourage fIuid intake, high fiber diet
and daiIy exercise
5. DO NO% administer if acute abdominaI
condition Iike appendicitis is present
6. Advise to change position sIowIy and
avoid hazardous activities because of
potentiaI dizziness
IMPLEMEN%A%ION
7. Record intake and output to assess
fIuid aIteration
8. If possibIe, observe the character of
stooIs
9. Caution the patient that chronic use
may promote dependence and use
during pregnancy may cause uterine
cramping and Vitamin deficiency
EVALUA%ION of drug effectiveness
1. EvaIuate reIief of GI symptoms,
absence of staining and increased
evacuation of GI tract
2. For LactuIose: decreased ammonia
3. omal bowel fucntion is restored
The Anti-diarrheals
%hese are agents used to caIm the
irritation of the GI% for the symptomatic
reIief of diarrhea
GeneraI CIassifications
1. LocaI anti-motiIity
2. LocaI refIex inhibition
3. CentraI action on the CNS
The Anti-diarrheals
%ype Prototype Action
LocaI refIex
inhibitor
Bismuth
subsaIicyIate
LocaIIy coats the Iining
of the GI% to soothe
irritation
LocaI anti-
motiIity
Loperamide
DirectIy inhibits the
intestinaI muscIe
activity to $LOW
peristalsis
CentraI acting
agent
Opium
derivatives
(paregoric)
$tops IT spasm b
$ action
linical ndications of drug use
ReIief of symptoms of acute and
chronic diarrhea
Reduction of fecaI voIume discharges
from iIeostomies
Prevention and treatment of traveIer's
diarrhea
ontraindications of anti-diarrheal
Use
Poisoning
Drug allerg
I obstruction
Acute abdominal conditions
Pharmacokinetics: Side effects
onstipation
ausea, vomiting
Abdominal distention and discomfort
TOXI MEAOLO
Nursing process and anti-diarrheals
ASSESSMEN%
Nursing History - EIicit history of drug
aIIergy, conditions Iike poisoning, GI
obstruction and acute abdominaI
conditions
PhysicaI Examination- AbdominaI
examination
Laboratory test- eIectroIyte IeveIs
NURSING DIAGNOSIS
AIteration in boweI pattern
AIteration in comfort: pain
IMPLEMEN%A%ION
1. Monitor patient response within 48
hours. Discontinue drug use if no
effect
2. Provide comfort measures for pain
3. Provide teaching regarding its short
term use onIy
EVALUA%ION
1. Monitor effectiveness of drug- RELIEF
of diarrhea
2. Monitor adverse effects, effectiveness
of pain measures and effectiveness of
teaching pIan
metics and Anti-emetics
Emetic Agent
$rup of Ipecac
Anti-emetics
1. Phenothiazines
2. Non-phenothiazines
3. AntichoIinergics/Antihistamines
4. Serotonin receptor BIockers
5. MisceIIaneous
MT
Prototype: Ipecac Syrup
MT
Pharmacodynamics
Ipecac syrup irritates the GI mucosa
IocaIIy, resuIting to stimuIation of the
vomiting center
It acts within 20 minutes
MT
CIinicaI Use of ipecac
%o induce vomiting as a treatment for
drug overdose and certain poisonings
MT
Contraindications of Ipecac use
Ingestion of CORROSIVE chemicaIs
Ingestion of petroIeum products
Unconscious and convuIsing patient
MT
Pharmacokinetics: side effects of Ipecac
Nausea
Diarrhea
GI upset
MiId CNS depression
ARDIOTOXIITY if large amounts are
absorbed in the bod
Nursing process and the
MT
ASSESSMEN%
Nursing History- eIicit the exact nature
of poisoning
PhysicaI Examination- CNS status and
abdominaI exam
MT
IMPLEMEN%A%ION
1. Administer to conscious patient onl
2. Administer ipecac as soon as
possibIe
3. Administer with a large amount of
water
4. Vomiting shouId occur within 20
minutes of the first dose. Repeat the
dose and expect vomiting to occur
with 20 minutes
MT
IMPLEMEN%A%ION
5. Provide comfort measures Iike ready
access to bathroom, assistance with
ambuIation
6. Offer support
MT
EVALUA%ION
1. EvaIuate patient response within 20
minutes of drug ingestion
2. Monitor for adverse effects
3. EvaIuate effectiveness of comfort
measures and teaching pIan
ANT-MTS
%hese are agents used to manage
nausea and vomiting
%hey act either IocaIIy or centraIIy
In generaI, they may inhibit the
chemoreceptor trigger zone in the
meduIIa by bIocking DOPAMINE
receptor
Others act by decreasing the sensitivity
of the vestibuIar apparatus
ANTMTS
Anti-emetic types Common exampIes
Phenothiazines ProchIorperazine,
Promethazine
Non-phenothiazines MetocIopramide
AntichoIinergics and
Antihistaminics
MecIizine, bucIizine
Serotonin Receptor
bIockers
setron"- doIasetron
MisceIIaneous DronabinoI, hydroxyzine
ANTMTS
%ypes Pharmacodynamics
Phenothiazines
CentraIIy bIock the vomiting center in
the meduIIa
Non-phenothiazine
Reduces the responsiveness of the
nerve ceII in the meduIIa; aIso bIocks
the dopamine receptors
AntichoIinergics
BIock the transmission of the impuIses
to the meduIIa
Serotonin receptor
bIockers
CentraIIy and IocaIIy inhibits the
serotonin receptors
MisceIIaneous
Act in the CNS , either in the meduIIa or
in the cortex
ANTMTS
%ypes CIinicaI Use
Phenothiazines
N/V associated with
anesthesia, intractabIe
hiccups
Non-phenothiazine
N/V associated with chemicaI
stimuIation
AntichoIinergics
N/V associated with motion
sickness
Serotonin-receptor
BIockers
N/V associated with
chemotherapy
MisceIIaneous N/V associated with
chemotherapy
ANTMTS
Indications
1. Prevention and treatment of vomiting
2. Motion sickness
ANTMTS
Contraindications
1. Severe CNS depression
2. Severe Iiver dysfunction
ANTMTS
Pharmacokinetics:
OraI absorption is good if vomiting is
not present
IV drugs can be given if vomiting is
active
Most drugs are metaboIized in the
Iiver excreted in the kidneys
ANTMTS
Pharmacokinetics: Side-effects
1. PHOTHO$E$ITIVITY
2. Drowsiness, dizziness, weakness and
tremors and DEHYDRATO
3. Phenothiazines autonomic anti-
cholinergic effects Iike dry mouth,
nasaI congestion and urinary
retention
MetocIopramide EPS due to dopamine
receptor bIockage
Nursing Process and the
ANTMTS
ASSESSMEN%
Nursing History- eIicit aIIergy,
impaired hepatic function and CNS
depression
PhysicaI Examination- CNS status and
abdominaI examination
Laboratory test- Liver function studies
ANTMTS
NURSING DIAGNOSIS
1. AIteration in comfort: pain
2. High risk for injury
3. KnowIedge deficit
ANTMTS
IMPLEMEN%A%ION
1. Assess patient's intake of other drugs
that may cause dangerous drug
interaction
2. Emphasize that this is given on a
short term basis
ANTMTS
MPMNTATON
3. Provide comfort and safety measures
Advise to change position sIowIy
Avoid hazardous activities
Provide mouth care and ice chips
Monitor for dehydration and offer fIuids if
it occurs
ANTMTS
IMPLEMEN%A%ION
4. Protect from sun exposure
Sunscreens
Protective covering
5. Provide heaIth teaching
ANTMTS
'AUATON
1. Monitor for the drug effectiveness
ReIief of nausea and vomiting
2. Monitor for adverse effects
3. valuate effectiveness of comfort
measures and teaching plan

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