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Drug Study

Drug Study

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Published by Zyryll Laoan

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Published by: Zyryll Laoan on Jan 17, 2011
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04/27/2012

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Clonidine
(
Catapres
) is amedicationused to treat several medical conditions. It is a direct-acting
2
 adrenergic agonistand animidazoline. MECHANISMClonidine treats high blood pressure by stimulating
2
receptorsin the brain, which decreasescardiacoutputandperipheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic
2
receptors in thevasomotor center in thebrainstem. This binding decreases presynaptic calciumlevels, and inhibits the release of norepinephrine. The net effect is a decrease in sympathetic tone.Is has also been hypothesised that the antihypertensive effect of clonidine is in fact due to agonism ontheimidazoline receptor which mediates the sympatho-inhibitory actions of imidazolines to lower bloodpressure. ADVERSE EFFECTThis drug may cause lightheadedness, dry mouth, dizziness, or constipation. Clonidine may also causehypotension Clonidine also has peripheral alpha agonist effects, which can lead to hypertension. These effects areseen during an overdose in children, where after taking clonidine their blood pressure increases. As theclonidine is eliminated by the body the peripheral effects wear off and the central hypotensive effectsbecome visible. Both the hypertensive and hypotensive effects can be harmful
Losartan
is anangiotensin II receptor antagonistdrug used mainly to treat high blood pressure(hypertension). Losartan was the first angiotensin II receptor antagonist to be marketed. It is currentlymarketed byMerck & Co.under thetrade name 
Cozaar 
. As of 2010 Losartan is now available ingeneric form.MECHANISMLosartan is a selective, competitive Angiotensin II receptor type 1(AT
1
) receptor antagonist, reducing theend organ responses to angiotensin II. Losartan administration results in a decrease in total peripheralresistance (afterload) and cardiac venous return (preload) All of the physiological effects of angiotensin II,including stimulation of release of aldosterone, are antagonized in the presence of losartan. Reduction inblood pressure occurs independently of the status of therenin-angiotensin system. As a result of losartandosing, plasma renin activity increases due to removal of the angiotensin II feedback.
Diazepam
first marketed as
Valium
byHoffmann-La Roche, is abenzodiazepine derivative drug. It is commonly used for treatinganxiety,insomnia,seizuresincludingstatus epilepticus,muscle spasms, restless legs syndrome,alcohol withdrawal,benzodiazepine withdrawalandMénière's disease. It may also be used before certain medical procedures (such asendoscopies) to reduce tension and anxiety,and in some surgical procedures to induceamnesia. It possessesanxiolytic,anticonvulsant,hypnotic, sedative,skeletal muscle relaxant, andamnesticpropertiesThe pharmacological action of diazepam enhances the effect of the neurotransmitter GABA by binding to the benzodiazepine site on theGABA
 A
 receptor leading tocentral nervous systemdepressionDiazepam has also been used as a recreational drug. Adverse effects of diazepam includeanterograde amnesia(especially at higher doses) andsedationas well asparadoxical effectssuch as excitement, rage or worsening of seizures in epileptics.Benzodiazepines also can cause or worsendepression.Long-term effects of benzodiazepinessuch as diazepam includetolerance,benzodiazepine dependenceas well as abenzodiazepine withdrawal
 
syndromeupon dose reduction; additionally after cessation of benzodiazepinescognitivedeficits may persist for at least 6 months and may not fully return to normal, however it was suggested that longer than6 months may be needed for recovery from some deficits Diazepam also has abuse potential and cancause serious problems of addiction. Urgent action by National Governments to improve prescribingpractices has been recommended.CONTRAINDICATIONS:Use of diazepam should be avoided, when possible, in individuals with the following conditions:
[45]
 
y
  Ataxia 
y
Severehypoventilation 
y
Acute narrow-angleglaucoma 
y
Severehepaticdeficiencies (hepatitisand liver cirrhosisdecrease elimination by a factor of 2)
y
Severerenaldeficiencies (e.g. patients ondialysis)
y
Liver disorders
y
Severe respiratory disorders
y
Severesleep apnea 
y
Severedepression, particularly when accompanied by suicidal tendencies
y
 Psychosis 
y
 Pregnancyor breast feeding 
y
Caution required in elderly or debilitated patients
y
 Comaor shock
y
Abrupt discontinuation of therapy
y
Acute intoxication withalcohol,narcotics, or other psychoactive substances (with the exception of  somehallucinogens, where it is occasionally used as a treatment for overdose)
y
History of alcoholor drug dependence 
y
 Myasthenia gravis, or MG, anautoimmune disorder causing marked fatiguability.
y
 Hypersensitivityor allergyto any drug in thebenzodiazepineclass SIDE EFFECT Diazepam has a range of side-effects that are common to most benzodiazepines. Mostcommon side-effects include:
y
Suppression of REM sleep 
y
Impaired motor function
o
Impaired coordination
o
Impaired balance
o
 Dizzinessand nausea
y
 Depression
[54]
 
y
 Reflex tachycardia Less commonly paradoxical side-effects can occur and include nervousness, irritability, Diazepam mayimpair the ability to drive vehicles or operate machinery. The impairment is worsened by consumption of alcohol, because both act as central nervous system depressantsDuring the course of therapy, tolerance to the sedative effects usually develops, but not to the anxiolyticand myorelaxant effectsMOA
 
Diazepam is a benzodiazepine that binds to a specific subunit on theGABA
 A
receptor at a site that isdistinct from the binding site of theendogenousGABA molecule. TheGABA
 
 A
receptor is an inhibitorychannel which, when activated, decreases neuronal activity. Benzodiazepines do not supplement for theneurotransmitter GABA, rather benzodiazepines such as diazepam bind to a different location on theGABA
 A
receptor with the result that the effects of GABA are enhanced. Benzodiazepines cause anincreased opening of the chloride ion channel when GABA binds to its site on the GABA
 A
receptor leadingto more chloride ions entering the neuron which in turn leads to enhanced central nervous systemdepressant effects. The muscle relaxant properties of diazepam are produced via inhibition of polysynapticpathways in the spinal cord.
E
someprazole
is aproton pump inhibitor (brand names
Sompraz
,
Zoleri
,
Nexium
,
Lucen
,
E
sopral
;
Axagon
in Italy,
Nexiam
in Belgium and South Africa) developed and marketed by AstraZenecawhich is used in the treatment of dyspepsia,peptic ulcer disease(PUD), gastroesophageal reflux disease(GORD/GERD) andZollinger-Ellison syndrome. Esomeprazole is the
-enantiomer of omeprazole(marketed as Losec/Prilosec), and AstraZeneca claims improvedefficacyof this single enantiomer product over theracemicmixture of omeprazole. However, this greater efficacy has been disputed, with some claiming it offers no benefit from itsolder form.SIDE EFFECTCommon side effects include headache, diarrhea, nausea, gas, decreased appetite,constipation, dry mouth, and abdominal pain. More severe side effects are severe allergicreactions, chest pain, dark urine, fast heartbeat, fever, paresthesia, persistent sore throat,severe stomach pain, unusual bruising or bleeding, unusual tiredness, and yellowing of the eyesor skinProton pump inhibitors may be associated with a greater risk of hip fracturesandclostridiumdifficile-associated diarrhea Patients are frequently administered the drugs in intensive care as aprotective measure against ulcers, but this use is also associated with a 30% increase inoccurrence of pneumonia.
M
etronidazole
is anitroimidazole antibioticmedication used particularly for anaerobic bacteria  andprotozoa. Metronidazole is an antibiotic, amebicide, and antiprotozoal.
[1]
It is the drug of choice for first episodes of mild-to-moderate
Clostridium difficile
infection.
[2]
It is marketed byPfizer under the trade name
F
lagyl
in the US, bySanofi-Aventisglobally under the sametradename
F
lagyl
, in Pakistan it is also available with the brand name of 
Nidagyl
manufacturedand marketed by Star Laboratories. In Thailand it is marketed as
M
epagyl
by Thai NakhornPatana. They are also marketed in UK by Milpharm Limited.MOAMetronidazole, taken up by diffusion, is selectively absorbed byanaerobic bacteriaandsensitiveprotozoa. Once taken up by anaerobes, it is non-enzymatically reduced by reactingwith reducedferredoxin, which is generated by pyruvate oxido-reductase. This reduction causesthe production of toxic products to anaerobic cells, and allows for selective accumulation inanaerobes.

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