You are on page 1of 23

a) Pharmacological class : NSAID Non selective inhibitors of the isoenzymes (COX-1 and COX-2

b) Mechanism of Action : Ibuprofen is a non-selective inhibitor of cyclooxygenase, an
enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. Its
pharmacological effects are believed to be due to inhibition cylooxygenase-2 (COX-2)
which decreases the synthesis of prostaglandins involved in mediating inflammation,
pain, fever and swelling. Antipyretic effects may be due to action on the hypothalamus,
resulting in an increased peripheral blood flow, vasodilation, and subsequent heat
dissipation. Inhibition of COX-1 is thought to cause some of the side effects of ibuprofen
including GI ulceration.
c) Pharmacologic effects :
It decreases the synthesis of prostaglandins involved in mediating inflammation, pain,
fever and swelling. Antipyretic effects may be due to action on the hypothalamus,
resulting in an increased peripheral blood flow, vasodilation, and subsequent heat
d) Therapeutic uses (indications) : For symptomatic treatment of rheumatoid arthritis,
juvenile rheumatoid arthritis and osteoarthritis. May be used to treat mild to moderate
pain and for the management of dysmenorrhea. May be used to reduce fever. Has been
used with some success for treating ankylosing spondylitis, gout and psoriatic arthritis.
May reduce pain, fever and inflammation of pericarditis. May be used IV with opiates to
relieve moderate to severe pain. Ibuprofen lysine may be used IV to treat patent ductus
arteriosus (PDA) in premature neonates.
e) Adverse Effects : Common adverse effects include: nausea, dyspepsia,
gastrointestinal ulceration/bleeding, raised liver enzymes, diarrhea, constipation,
epistaxis, headache, dizziness, rash, salt and fluid retention, and hypertension.
Infrequent adverse effects include: esophageal ulceration, heart failure, MI,
hyperkalemia, renal impairment CA, confusion, and bronchospasm. Ibuprofen can
exacerbate asthma, sometimes fatally. In skin ibuprofen has been associated with the
onset of bullous pemphigoid. it has been reported to be a photosensitizing agent and
extremely rare cause of the autoimmune disease Stevens-Johnson syndrome. It can
also cause erectile dysfunction or Miscarriage and Rhabdomyolysis, especially in people
with with high blood cholesterol, hyperlipidemia, high blood pressure, depression.
f) Contraindications : IBU tablets are contraindicated in patients with known
hypersensitivity to Ibuprofen. Should not be given to patients who have experienced
asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe,
rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
IBU tablets are contraindicated for the treatment of peri-operative pain in the setting of
coronary artery bypass graft (CABG) surgery.
g) Pharmacography : Cap 200mg, tab40/200/400/600/800mg, IV 100mg/ml
h) Prescription
Dg/ Rheumatoid arthritis
Rp/Ibuprofen 200mg
D.s. orally 3 tabs per day for 14days

a) Pharmacological class : NSAID
b) Mechanism of Action : Acetaminophen is thought to act primarily in the CNS,
increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1,
COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs,
acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no
peripheral anti-inflammatory affects. Studies suggest that acetaminophen selectively
blocks COX-3. Its exact mechanism of action is still poorly understood.
c) Pharmacologic effects : Acetaminophen inhibits prostaglandin synthesis in the CNS.
This explains its antipyretic properties from direct effects on the heat-regulating centers
of the hypothalamus resulting in peripheral vasodilation, sweating and hence heat
dissipation and analgesic properties. It has less effect on cyclooxygenase in peripheral
tissues, which accounts for its weak anti-inflammatory activity and does not affect
platelet function or increase blood clotting time.
d) Therapeutic uses (indications) : Acetaminophen is a suitable substitute for the
analgesic and antipyretic effects of aspirin for those patients with gastric complaints,
those in whom prolongation of bleeding time would be a disadvantage, or those who do
not require the anti-inflammatory action of aspirin. Acetaminophen is the
analgesic/antipyretic of choice for children with viral infections or chickenpox (recall that
aspirin increases the risk of Reye's syndrome and does not antagonize the uricosuric
agents probenecid or sulfinpyrazone and, therefore, may be used in patients with gout
who are taking these drugs.
e) Adverse Effects : Skin rash and minor allergic reactions occur infrequently. There may
be minor alterations in the leukocyte count, but these are generally transient. Renal
tubular necrosis and hypoglycemic coma are rare complications of prolonged, largedose therapy. With large doses of acetaminophen Hepatic necrosis, a very serious and
potentially life-threatening condition, can result. Renal tubular necrosis may also occur.
f) Contraindications : Liver Failure, Liver Problems, Serious Kidney Problems
g) Pharmacography :Tabs 500mg/1000mg, capsule, liquid suspension, suppository, IV,IM

h) Prescription
Dg/ fever
Rp/Paracetamol 500mg
D.s. orally 1 tab every 6 hours for 3 days

producing an anticoagulant effect with a prolonged bleeding time.  External applications: used topically to treat corns. Low doses are used prophylactically to: o Reduce the risk of recurring transient ischemic attacks and stroke or death. rheumatic fever. . Commonly treated conditions requiring analgesia include headache.  The analgesic effect is due to the decrease of prostaglandin synthesis preventing sintetization of pain receptors to both mechanical and chemical stimuli. It also depress pain stimuli at subcortical sites (thalamus and hypothalamus).  Cardiovascular applications: used to inhibit platelet aggregation. and Rheumatoid Arthritis. and myalgia. inhibiting prostaglandin formation. This ability gives its anti-inflammatory. and analgesic uses: used in the treatment of gout. calluses. c) Pharmacologic effects :  anti-inflammatory and antirheumatic action: modulates those aspects of inflammation in which prostaglandins act as mediators  analgesic action: used mainly for the management of pain of low to moderate intensity arising from musculoskeletal disorders  antipyretic action: lowers the body temperature of febrile patients by increasing heat dissipation as a result of peripheral vasodilation and sweating.  Kidney effects: causing retention of sodium and water and may cause edema and hyperkalemia. osteoarthritis. o Reduce the risk of death in those having an acute myocardial infarction. d) Therapeutic uses (indications) :  Anti-inflammatory. o Reduce the risk of recurrent nonfatal myocardial infarction and/or death o Reduce the risk of myocardial infarction and sudden death in patients with chronic stable angina pectoris. antipyretic. and warts.  The first two are due to the blockade of prostaglandin synthesis at the thermoregulatory centers in the hypothalamus and at peripheral target sites.  Platelet effects: platelet aggregation (the first step in thrombus formation) is reduced.  Respiratory effects: increasing alveolar ventilation.  Gastric effects: increases acid secretion and decreases mucus formation.a) Pharmacological class : NSAID b) Mechanism of Action : IRREVERSIBLY inactivates cyclooxygenase. antipyretic and analgesic effects. arthralgia.

Blood: Should not be taken for at least one week prior surgery. h) Prescription Dg/ Muscular pain Rp/ Acetylsalicylic acid/Aspirine Nr. fulminating hepatitis with cerebral edema. g) Pharmacography : Oral or rectal administration. or angioedema. only at higher doses do these drugs show anti-inflammatory activity.  Hypersensitivity: causing urticaria. nausea.e) Adverse effect :  Gastrointestinal: Epigastric distress. vomiting and microscopic GI bleeding. orally 1 tab every 12h for 5 days .  Pregnancy and breast can cause respiratory depression and a combination of uncompensated respiratory and metabolic acidosis.s. which is an often fatal. especially encountered in children.  Blood: inhibition of platelet aggregation and a prolonged bleeding time  Respiratory: In toxic doses.  Reye's syndrome: when given during viral infections. X D. it has been associated with an increased incidence of Reye's syndrome. bronchoconstriction. For example. f) Contraindications :   Gastrointestinal: not to take with empty stomach. two 325-mg. Aspirin exhibits analgesic activity at low doses.

 Kidney effects: increases water and sodium retention.  81% increase in incidence of upper gastrointestinal complications: perforations.  Severe hepatic impairment.a) Pharmacological class : NSAID b) Mechanism of Action : selective noncompetitive reversible inhibitor of cyclooxygenase-2 (COX-2) enzyme that synthetizes prostaglandin and thromboxane. obstructions or bleeds. Late pregnancy and breast feeding g) Pharmacography : 50. e) Adverse Effects :  37% increase in incidence of major vascular events: non-fatal myocardial infarction. d) Therapeutic uses (indications) :  Relief and management of rheumatoid arthritis and osteoarthritis  acute pain  primary dysmenorrhea  Familial adenomatous polyposis. non-fatal stroke or death from a vascular cause.  Gastric effects: increases acid gastric secretion and decreases mucus production. XXX D. c) Pharmacologic effects :  anti-inflammatory and antirheumatic.  History of asthma or urticaria. 400mg capsule h) Prescription Dg/ Osteoarthritis Rp/ Celecoxib 200mg Nr. Skin reactions. Hematologic events: anemia may occur. 100. 200.  Renal disease.s.  Analgesic action: for acute pain.   f) Contraindications :  hypersensitivity. 1 per 24h after meal for 1 month .

f) contraindications : • Active ulcers. followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling. jaundice (yellowing of the skin or eyes).5. XX D.  black. itching. tenderness.  urinating less than usual or not at all. • Hepatic/renal insufficiency • Pregnancy and breast feeding. swelling in your face or tongue. skin pain. bloody. 15 mg. upper stomach pain. slurred speech. In low dosages it shows selectivity for COX2. problems with vision or balance. and stiffness associated with arthritis. Oral Suspension: 7. c) Pharmacologic effects :  analgesic  antipyretic. weakness.  nausea. • Hypersensitivity • asthma g) Pharmacography : Tablets: 7.  anti-inflammatory. 1 per 12h after meal for 10 days . fever. shortness of breath.  Severe skin reaction. dark urine.s.5 mg/ml h) Prescription Dg/ Arthritis Rp/ Meloxicam 7. burning in your eyes. loss of appetite.a) Pharmacological class : NSAID b) Mechanism of Action : The inhibition of cyclooxygenase leads to the inhibition of prostaglandin synthesis. or tarry stools  coughing up blood or vomit that looks like coffee grounds. e) Adverse Effects :  chest pain.  swelling or rapid weight gain.5mg Nr. sore throat. swelling. d) Therapeutic uses (indications) : Indicated to relieve pain. clay-colored stools.

 Antidiarrheal e) adverse effects:  Nausea  Diarrhoea  Constipation. orally after meal 3 times per day for a week . o Antidiarrheal: decrease fluidity of stools. d) Therapeutic uses:  antiacid  antiurolithc  antihyperphosphatemic  antihypocalcemic. o Antihypocalcemic: increase the release of calcium from bone. suspension h) Prescription : Dg/ GERD Rp/ Maalox suspension Nr. I D. o Antihyperphosphatemic: reduce serum phosphate levels. increasing pH and increases intra-esophageal pH and decrease pepsin activity c) Phamacologic effects: o antacid o antiurolithic: reduction of phosphates in urine preventing urinary stones.a) Pharmacological class : Non absorbed antacid b) Mechanism of Action : neutralize or buffer stomach acid with no direct effect on its output.s. f) contraindications: Not to be taken with iron preparates or antibiotics g) Parmacography: Tabs 400-800mg chewed.

when hydrolyzed to salicylic acid. Both bismuth subsalicylate and the intestinal reaction products.a) Pharmacological class : Mucosal protective agent b) Mechanism of Action : It forms a protective coat. e) Adverse Effects : It can cause a black tongue and black stools in some users of the drug. bismuth subsalicylate binds toxins produced by Escherichia coli. It can also cause a black tongue and black stools in some users of the drug. XXX D. suspension h) Prescription Dg/ H-Pylori Rp/ Bismuth Subsalicylate tabs Nr. suppository. the exact mechanism has not been determined. diarrhea.s. indigestion. For the same reason. d) Therapeutic uses (indications) : Most important use is to treat H-pylori in a combination with other drugs. As an antacid. and the discoloration seen is temporary and harmless. by inhibiting synthesis of a prostaglandin responsible for intestinal inflammation and hyper motility. As an antidiarrheal. upset stomach. c) Pharmacologic effects: Bismuth subsalicylate displays anti-inflammatory action (due to salicylic acid) and also acts as an antacid and mild antibiotic. orally 3 tabs per day after food . and other temporary discomforts of the stomach and gastrointestinal tract. as epidemiologic evidence points to an association between the use of salicylate-containing medications during certain viral infections and the onset of Reye's syndrome. Bismuth subsalicylate may exert its antidiarrheal action not only by stimulating absorption of fluid and electrolytes across the intestinal wall (anti-secretory action) but also. In addition. bismuth oxychloride and bismuth hydroxide. liquid. f) Contraindications: Children should not take medication with bismuth subsalicylate while recovering from influenza or chicken pox. bismuth has weak antacid properties. This discoloration is temporary and harmless. Bismuth sulfide is a highly insoluble black salt. when it combines with trace amounts of sulfur in saliva and the colon to form bismuth sulfide. when it combines with trace amounts of sulfur in their saliva and gastrointestinal tract. g) Pharmacography : tabs. it is typically recommended that nursing mothers not use medication containing bismuth subsalicylate because small amounts of the medication are excreted in breast milk and pose a theoretical risk of Reye's syndrome to nursing children. heartburn. Also used to treat nausea. Also constipation and dry mouth are possible. are believed to have bactericidal action. Long-term use (greater than 6 weeks) may lead to accumulation and toxicity.

Increase risk of pneumonia. This is achieved by two ways: a. Reduction of vitamin B12 absorption. Acute stress ulcers. 1 tab every day for 30 days. GERD. e. c. f) Contraindications: a. Tablet: 25. Peptic ulcers. Preoperatively reduces risk of aspiration pneumonia. b. d. d) Therapeutic uses: a.s. e. c. c. Increase risk of infectious diarrhea. Intravenous solution 1mg/ml or 25mg/ml b. Reduction of drugs absorption requiring acidic stomach. Hypersensitivity.XXX D. d. Histamine released by enterocromoffin-like cells in the stomach is blocked from binding on parietal cell H2 receptors. Orally. . b) Mechanism of action: competitively blocks the action of histamine on parietal cells in the stomach decreasing their acid production. Fungal sepsis. e) adverse effects: a. Food or drug allergies.a) Pharmacological class: H2 receptor antagonist. 300mg. Syrup: 15mg/ml h) Prescription Dg/ Peptic ulcer Rp/Ranitidine tabl. 300mg Nr. Acute renal/cardiac failure. c) Pharmacologic effects: inhibit gastric acid secretion induced by histamine or gastrin. g) Pharmacography: a. acetylcholine) have a reduced effect on parietal cells when H2 receptors are blocked. Other substances that promote acid secretion (as gastrin. b. 75 150. b. f. b. Co-administered with NSAIDs to reduce risk of ulceration.

20 mg Nr XXI D. Orally. XIV D. c) Pharmacologic effects: Inhibits both basal and stimulated gastric acid secretion. 40mg b) Prescription : Combined for H. Low vitamin B12 (acid is required for its absorption).s1. 40 mg. Pylori + Rp1/Omeprazole. f) Contraindications: When patient takes anticoagulant therapy g) Pharmacography: Capsule: 10. XIV D.pylori together with antimicrobial regimens  Long-term treatment of pathologic hypersecretory conditions. Tablets: 20mg. Pylori treatment Dg/ Ulcer H.a) Pharmacological class: Proton pump inhibitor (antisecretory agent) b) Mechanism of action: It binds the proton pump of the parietal cell supressing secretion of hydrogen ions into the gastric lumen and thereby supressing secretion of gastric acid. 1tab/day/21days Rp2/Amoxilcilin cap 500mg Nr. tab. e) Adverse effects: Increased concentrations of bacteria in stomach.  GERD  Reduce risk of bleeding from NSAIDs.s Orally 1 tab per 8 hours for 2 weeks . Increased diarrhea.s Orally 1 cap per 8 hours for 2 weeks Rp3/Metronidazole tab 250mg Nr. 20. d) Therapeutic uses:  Treating erosive esophagitis and active duodenal ulcer and eradicate H.

Both these effects are antagonized by theophylline  Anti-inflammatory action (type IV PDE) low-dose theophylline inhibits late response to antigenic challenge  increases in CD4 and CD8 lymphocytes c) Pharmacologic effects :  In Central Nervous System : o increased alertness. hypothyroidism. pulmonary edema. reduced tubular sodium reabsorption)  Smooth Muscle: Major Effect in Bronchodilaton d) Therapeutic uses (indications) :  Most effective xanthine bronchodilator  Relieves airway obstruction: o in acute asthma and COPD o reduces symptoms severity e) Adverse Effects :  Particularly at higher doses. nausea and vomiting are the early events  cardiac arrhythmias  seizures and even death f) Contraindications : caution if seizure disorder. 10 mg/kg body weight/day or more. are significant  GI symptoms. 300mg.nervousness/insomnia o very high methylxanthine doses: medullary stimulation. convulsions o Primary side effect in patients requiring aminophylline (large doses) for control of asthma: nervousness & tremor  In Cardiovascular : o direct positive chronotropic o direct enhanced myocardial contractility  Gastrointestinal Tract: o enhanced secretion of gastric acid and digestive enzymes o stimulates secretion (secretagogue)  Renal: weak diuretics. not therapeutically important (increased glomerular filtration. orally 1 tab/day after food for 30days . arrhythmias. cor pulmonale. if sepsis or multi-organ failure g) Pharmacography : tabs 100mg. 200mg.s. reduced fatigue o in more sensitive individuals: caffeine -. 600mg h) Prescription : Dg/ COPD Rp/ Theophylline 100mg Nr.a) Pharmacological class : Methylxanthines b) Mechanism of Action :  It inhibits phosphodiesterase and results in increased intracellular cAMP which may account for cardiac stimulation and smooth muscle relaxation  It inhibits the receptors of adenosine (modulators of adenylyl cyclase activity) Adenosine is responsible for the isolated airway smooth muscle contraction and histamine release from lung cells. XXX D. hepatic impairment.

Also used in the treatment of Allergic rhinitis. wheezing and chest tightness f) Contraindications : The drug is effective only for asthma prophylaxis. and vernal keratitis. o Is also effective in reducing symptoms of allergic rhinitis & hay fever (allergic condition ) d) Therapeutic uses (indications) : For the management of patients with bronchial asthma (not acute). chemical anaphylaxis mediators more effective in reducing seasonal increases in bronchial reactivity (allergic asthma) but less effective when compared with inhaled corticosteroids. g) Pharmacography : .Nasal solution: 40 mg/ml . e) Adverse Effects : Throat irritation. cough. Nasally 1 time in each nostril 30 mins before meal every 12h . vernal keratoconjunctivitis. not treatment of an acute asthma attack.Oral solution: 100 mg/5 ml . I D.Aerosol spray for inhalation: 800 mcg/spray . mouth dryness. vernal conjunctivitis.s.Ophthalmic solution: 4% .mast cells specific (cromolyn -minimal mediator released inhibition on human basophils) o inhibition of late response to antigens (eosinophils) c) Pharmacologic effects : o Blocks bronchoconstriction due to antigen inhalation o Blocks aspirin-induced bronchoconstriction or bronchoconstriction induced by environmental agents o Reduces bronchodilators medication requirements and symptomatic severity in patients with perennial asthma o In chronic treatment appears to decrease the bronchial hyper-reactivity: airway protection against inflammatory.Solution for nebulization: 10 mg/ml h) Prescription Dg/ Allergic Rhinitis Rp/ Cromolyn Sodium nasal sol 40mg/ml Nr. Hayfever .a) Pharmacological class : antihistaminic or Anti-asthmatic or anti-inflammatory agent b) Mechanism of Action :  Alters function of delayed chloride channels (best demonstrated for nedocromil) and inhibits cell activation  And has Chloride-mediated channel effects: o inhibition of cough o inhibition of early response to antigens from mast cells and inhibits degranulation and release of histamine .

c) Pharmacologic effects : . Drowsiness is also a common side effect. in the human airway. viscous mucus. allergic rhinitis. e) Adverse Effects : Side effects include gastrointestinal disturbances. o For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet. CysLT1.s.a) Pharmacological class : Leukotriene receptor antagonist (LTRA) b) Mechanism of Action : Montelukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor. h) Prescription Dg/Chronic Asthma Rp/Montelukast 10mg Nr. hypersensitivity reactions. headaches. Anxious. f) Contraindications : Shouldn’t be administered if feeling restless. smooth muscle contraction. Involuntary Quivering. and enhanced secretion of thick. Nervous. exercise induced bronchospasm. and enhanced secretion of thick. Mood Changes. orally 1 tab every night . and urticaria. Abnormal Dreams. It inhibits the actions of LTD4at the CysLT1 receptor. viscous mucus. Depression. Its use is associated with a higher incidence of Churg–Strauss syndrome (whether or not this drug is 'unmasking' subclinical Churg– Strauss is as yet uncertain). Inflammation of Blood Vessels in the Skin. g) Pharmacography : o For adults and adolescents 15 years of age and older: one 10-mg tablet. sleep disorders. It is mainly used as a complementary therapy in adults in addition to inhaled corticosteroids. Prevents airway edema. preventing airway edema. Increased Eosinophils in the Blood. Hallucination. XXX D. o For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet or one packet of 4-mg oral granules. d) Therapeutic uses (indications) : Used for a number of conditions including asthma but not attacks. suicidal thoughts. smooth muscle contraction. and increased bleeding tendency. if they alone do not bring the desired effect. in addition to other generic adverse reactions.

interleukin-10.s. d) Therapeutic uses (indications) : Fluticasone propionate. and orally for the maintenance treatment of asthma as prophylactic therapy and for patients requiring oral corticosteroid therapy for asthma. and interleukin-12. In the management of asthma. Inhalatory. reduction in fibroblast proliferation. . Hypocortisolism (suppressed cortisol) can be expected as a result of sudden withdrawal from fluticasone propionate. reduction of complement components. blisters. pruritus. stuffy or runny nose. and 5. e) Adverse Effects : The topical drug has been associated with burning. 1 inhalation per 12h for 1 month. The anti-inflammatory actions of corticosteroids are also thought to involve inhibition of cytosolic phospholipase A2 (through activation of lipocortin-1 (annexin)) which controls the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. is used topically to relieve inflammatory and pruritic symptoms of dermatoses and psoriasis. and up-regulates anti-inflammatory mediators such as IkappaB [inhibitory molecule for nuclear factor kappaB1]. Candidiasis of mouth and throat is reported as a "very common" side effect. exacerbation of pruritus. specifically glucocorticoids b) Mechanism of Action : Binds to the glucocorticoid receptor. c) Pharmacologic effects : Fluticasone is an extremely potent vasoconstrictor and antiinflammatory agent. Severe hypersensitivity to milk proteins g) Pharmacography : o Aerosol for inhalation o Cream for Topical use o Powder for Respiratory (inhalation) o Spray for nasal use h) Prescription Dg/ Chronic Asthma Rp/Fluticasone propionate discus Nr. f) Contraindications : primary treatment of status asthmaticus or other acute episodes of asthma or COPD where intensive measures are required. dryness. atopic dermatitis. viral warts. and interference with the formation of scar tissue. the glucocorticoid receptor complexes down-regulates pro-inflammatory mediators such as interleukin 1. exacerbation of eczema. I D. binding with high affinity to glucocorticoid receptors (GR). impetigo. difficulty speaking. interference with leukocyte adhesion to the capillary wall. 3. erythema. sore or irritated throat and painful white patches in the mouth or throat. Unbound corticosteroids cross the membranes of cells such as mast cells and eosinophils. The results include alteration of transcription and protein synthesis. skin infection. Hoarseness is also common. and folliculitis. inhibition of histamine and kinin release.a) Pharmacological class : corticosteroids. reduction of collagen deposition. prevention of macrophage accumulation at inflamed sites. a medium-potency synthetic corticosteroid. intranasally to manage symptoms of allergic and non-allergic rhinitis. a decreased release of leukocytic acid hydrolases. infected eczema. There are also numerous side effects associated with the oral version of this medication including headache. skin irritation. stinging. Its effectiveness in inhaled forms is due to its direct local effect. reduction of capillary membrane permeability and subsequent edema.

The activity of this receptor is mediated by G proteins which normally activate adenylate cyclase.a) Pharmacological class: Synthetic Prostaglandin E Naturally occurring prostaglandin E2 is produced by mucosal cells of the stomach and duodenum.  Increased thickness of mucus layer. The significant cytoprotective actions of misoprostol are related to several mechanisms. Misoprostol is also commonly used for labor induction in missed miscarriage.  Enhanced mucosal blood flow as a result of direct vasodilatation. It inhibits gastric acid secretion and increases mucous and bicarbonate. fever. erosion and ulceration of the gastric mucosa may occur b) Mechanism of action: Misoprostol seems to inhibit gastric acid secretion by a direct action on the parietal cells through binding to the prostaglandin receptor. dyspepsia. g) Pharmacography: tabs 50 mcg. e) Adverse effects: Diarrhea. which may cause partial or complete abortions.Pharmacologic effects: Stimulates increased secretion of the protective mucus that lines the gastrointestinal tract and increases mucosal blood flow. mucosal blood flow and mucosal repair (cytoprotective effect) With inhibition of Prostaglandin E. 1 tabl every 8h for 10 days . and because its use in pregnancy has been associated with birth defects.  Improvement of mucosal regeneration capacity.  Replacement of prostaglandins that have been depleted as a result of various insults to the area. headache. These include:  Increased secretion of bicarbonate.  It prevents harmful agents from disrupting the tight junctions between the epithelial cells which stops the subsequent back diffusion of H+ ions into the gastric mucosa. 200mcg h) Prescription : Dg/Ulcer prophylaxis Rp/ Misoprostol 100mcg Nr.s. Misoprostol has also been shown to increase the amplitude and frequency of uterine contractions during pregnancy via selective binding to the EP-2/EP-3 prostanoid receptors c) . abdominal pain. thereby increasing mucosal integrity. d) Therapeutic uses: Indicated for patients at high risk for GI ulceration and bleeding and in those who take NSAIDs. 100mcg.XXX D. vomiting.Orally.  Stabilization of tissue lysozymes/vascular endothelium. and constipation. flatulence. nausea. The indirect inhibition of adenylate cyclase by Misoprostol may be dependent on guanosine5’-triphosphate (GTP).  Considerable decrease in the volume and pepsin content of the gastric secretions. f) Contraindications: Misoprostol should not be taken by pregnant women to reduce the risk of NSAID induced gastric ulcers because it increases uterine tone and contractions in pregnancy.

V Ds. c) Pharmacologic effects: Nitrates decrease coronary vasoconstriction or spasm and increase perfusion of the myocardium by relaxing coronary arteries. Flushing and can cause severe headaches. g) Pharmacography: Caps: 2. tab 0. bradycardia and syncope.5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells. or Levitra. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation. This stimulates the synthesis of cyclic guanosine 3'. they relax veins. d) Therapeutic uses: Nitroglycerin is used in the treatment of angina pectoris and perioperative hypertension. to treat hypertensive emergencies.5mg. 9mg Injectable: 0.5 mg Nr. In addition.a) Pharmacological class: Nitrate b) Mechanism of action: Nitroglycerin is converted to nitric oxide (NO). e) Adverse effects: Tolerance.5-5mg/ml Sublingual: 0. The combination of the two can lead to severe hypotension. severe hypotension. 1 tab when necessary . decreasing preload and myocardial oxygen consumption. to produce controlled hypotension during surgical procedures. 6. and to treat congestive heart failure associated with myocardial infarction. an active intermediate compound which activates the enzyme guanylate cyclase.5mg. f) Contraindications: It must not be used together with vasodilators that combat erectile dysfunction. circulatory collapse and death. Sublingually. Cialis. such as Viagra. eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber.5mg h) Prescription : Dg/ Angina Rp/ Nitroglycerin.

and/or peripheral vascular disease ( Black hypertensives respond well to calcium-channel blockers). These agents are useful in the treatment of hypertensive patients who also have asthma. 2.5mg h) Prescription : Dg/ Hypertension Rp/ Felodipine 10 mg Nr. c) Pharmacologic effects: Vascular smooth muscle relaxation and dilation mainly of arterioles. which further increases the cytosolic level of calcium. 1 tablet per day at breakfast. d) Therapeutic uses: Calcium-channel blockers have an intrinsic natriuretic effect and. for 1 month . Use cautiously with pregnancy. This triggers release of calcium from the sarcoplasmic reticulum and mitochondria. angina. do not usually require the addition of a diuretic. heart block (second and third degree). therefore.a) Pharmacological class: Calcium Channel Blockers b) Mechanism of action: The intracellular concentration of calcium plays an important role in maintaining the tone of smooth muscle and in the contraction of the myocardium. lactation. Hypotension f) Contraindications: Not to be administered in sick sinus syndrome. diabetes. XXX DS: Orally. Calcium enters muscle cells through special voltage-sensitive calcium channels. Flushing. impaired hepatic function. g) Pharmacography: Tablets: 10mg. Calcium-channel antagonists block the inward movement of calcium by binding to L-type calcium channels in the heart and in smooth muscle of the coronary and peripheral vasculature. e) Adverse effects: Tachycardia. 5mg.

It also may paradoxically increase ventricular rate in patients with Wolff-ParkinsonWhite syndrome because of accessory conduction pathways. in low blood pressure patients with systolic blood pressures below 90 mm Hg. f) Contraindications: In congestive heart failure. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue. 90mg. e) Adverse effects: hypotension. inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. supraventricular tachycardia. peripheral artery occlusive disease. in SA node or AV conduction disturbances. c) Pharmacologic effects: Dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue. 300mg Injection IV h) Prescription : Dg/ Hypertension Rp/ Diltiazem tab 90mg Nr LX Ds. diltiazem. impaired left ventricle function. 120mg. d) Therapeutic uses: Used in the treatment of hypertension. bradycardia. and/or interfering with the release of calcium from the sarcoplasmic reticulum. inhibiting ion-control gating mechanisms. 1 tab per 12h for 30 days . dizziness. g) Pharmacography: Caps: 120mg. 300mg Tablets: 30mg. 240mg. and some types of arrhythmia. bradycardia. angina pectoris. 180mg. 240mg. like verapamil. Diltiazem is relatively contraindicated in the presence of sick sinus syndrome.a) Pharmacological class: calcium channel blocker . 60mg.Benzothiazepines b) Mechanism of action: Possibly by deforming the channel. and flushing. Orally. and chronic obstructive pulmonary disease. 180mg.

dizziness. Calcium channels are also present in the smooth muscle that lines blood vessels. ecchymosis. hypotension. and constipation. heart failure. e) Adverse effects: Some possible side effects of the drug are bradycardia.Diphenylalkylamines b) Mechanism of action: The intracellular concentration of calcium plays an important role in maintaining the tone of smooth muscle and in the contraction of the myocardium. d) Therapeutic uses: It is used to treat angina.a) Pharmacological class: calcium channel blocker . Since calcium channels are especially concentrated in the sinoatrial and atrio-ventricular nodes. This has led to their use in treating hypertension and angina pectoris. Calcium-channel antagonists block the inward movement of calcium by binding to L-type calcium channels in the heart and in smooth muscle of the coronary and peripheral vasculature. Orally. Calcium enters muscle cells through special voltage-sensitive calcium channels. lightheadedness. galactorrhea. fatigue. f) Contraindications: Verapamil should be avoided in patients with congestive heart failure . nausea. thus protecting the ventricles from atrial tachyarrhythmias. and migraine headache.with atrioventricular block due to its negative inotropic (force of cardiac muscle contraction) and dromotropic (velocity of conduction) effects and in vasospamic angina. By relaxing the tone of this smooth muscle. calciumchannel blockers dilate the blood vessels. increased urination. these agents can be used to decrease impulse conduction through the AV node. headaches. swelling. g) Pharmacography: Tablets: 40mg – 80mg – 120mg 24h Capsules : 100mg – 120mg – 180mg – 200mg . dilation mainly of arterioles. is also used intra-arterially to treat cerebral vasospasm. This triggers release of calcium from the sarcoplasmic reticulum and mitochondria.240 mg – 300mg – 360mg h) Prescription : Dg/Hypertension Rp/ Verapamil cap 120mg Nr XXX Ds. which further increases the cytosolic level of calcium. supraventricular tachyarrhythmias. AV block. c) Pharmacologic effects: Verapamil is the least selective of any calcium-channel blocker and has significant effects on both cardiac and vascular smooth muscle cells and causes smooth muscle to relax. facial flushing. 1 tab per 24h .

s. tabl 50mg Nr. Orally. f) Contraindications: Metoprolol is contraindicated in patients with bradycardia < 45 beats/min. c) Pharmacologic effects: Reduction in resting heart rate. or moderate-to-severe cardiac failure. e) Adverse effects: Dizziness. and vision problems. ataxia.a) Pharmacological class: Selective β1 blocker b) Mechanism of action: Drug. unusual 100-fold less than those required to block beta-2 receptors. Cardioselective beta-blocker antagonizes beta-1 receptors. causing them to feel numb and cold. It may also reduce blood flow to the hands and feet. depression.24 sec) and systolic blood pressure < 100 mmHg. inhibiting sympathetic stimulation. cough. This cardioselectivity is thus most pronounced at low doses and is lost at high doses. systolic and diastolic blood pressure. g) Pharmacography: IV vials : 1mg/ml Tablets: 25mg – 50mg – 100mg – 200mg h) Prescription : Dg/Hypertension Rp/Metoprolol. dyslipidemia and polydipsia. erectile dysfunction (impotence). angina pectoris. May be used to treat supraventricular and tachyarrhythmias and as prophylaxis for migraine headaches. Due to the high penetration across the blood brain barrier. drowsiness. cardiac output. mental/mood changes. heart failure and mild to moderate hypertension. d) Therapeutic uses: For the management of acute myocardial infarction. fatigue. and reflex orthostatic hypotension. developed to eliminate the unwanted bronchoconstrictor effect (beta-2 effect) of propranolol seen among asthmatic patients. lipophilic beta blockers such metoprolol are more likely than other less lipophilic beta blockers to cause sleep disturbances such as insomnia and vivid dreams and nightmares. Other possible effects are sexual dysfunction. depression. at doses 50.XXX D. that preferentially blocks the beta-1 receptors. dyspnea. trouble sleeping. diarrhea. second and third degree heart block. significant first degree heart block (P-R interval ≥ 0. 1 tabl/day for 30 days . hair loss.

g. cardiac output.25 mg Tablets: 5mg – 10mg h) Prescription : Dg/Hypertension Rp/Bisoprolol-Hydrochlorothiazide. 20 mg and greater) bisoprolol may competitively block β2-adrenergic receptors in bronchial and vascular smooth muscle causing bronchospasm and vasodilation. β1-selective blockers prevent the release of renin. In addition.This results in a reduction of heart rate. a hormone produced by the kidneys that cause constriction of blood vessels. β1-adrenergic blocking agents such as bisopolol lower the heart rate and blood pressure and may be used to reduce workload on the heart and hence oxygen demands. Bronchospasms and low blood sugar because at high doses drug can be an antagonist for β2 adrenergic receptors located in lung and in liver. Orally. At higher doses (e. low blood sugar. if indicated). a diuretic and a digitalis-glycosid. g) Pharmacography: Tablets combined with diuretics : Bisoprolol-Hydrochlorothiazide 2. which is an undesired effect in congestive heart failure. tab 5-6. c) Pharmacologic effects: Activation of β1-receptors (located mainly in the heart) by epinephrine increases heart rate and the blood pressure causing the heart to consume more oxygen. and possibly reflex orthostatic hypotension. d) Therapeutic uses: Used to treat cardiovascular diseases such as hypertension. bronchospasms and bradycardia. as bisoprolol reduces also the muscular power of the heart. e) Adverse effects: Fatigue. Patients with compensated congestive heart failure may be treated with bisoprolol as a comedication (usually together with an ACE inhibitor. Bronchspasm due to blockage in lungs of β2 receptor and low blood sugar because of decreased stimulation of glycogenolysis and gluconeogenesis in the liver via β2 receptor. It is very important to start with low doses.5 or 5 or 10-6. . In patients with congestive heart failure. systolic and diastolic blood pressure. coronary heart disease. it reduces the need for and the consumption of oxygen of the heart muscle.XXX D. ischemic heart diseases and treatment of myocardial infarction after the acute event.25 mg Nr.a) Pharmacological class: Selective β1 blocker b) Mechanism of action: Bisoprolol selectively blocks catecholamine stimulation of β1adrenergic receptors in the heart and vascular smooth muscle. They are routinely prescribed in patients with ischemic heart disease. hypotension. They should be avoided in patients with a history of asthma or bronchospasm. arrhythmias. f) Contraindications: Beta-blockers can precipitate asthma and this effect can be dangerous.s. 1 tabl/day for 30 days .

Inhibiting the deactivation of bradykinin increases bradykinin levels and may sustain its effects by causing increased vasodilation and decreased blood pressure. renin cleaves circulating angiotensinogen to ATI.} d) Therapeutic uses: For the treatment of essential or renovascular hypertension (usually administered with other drugs. May be used to treat nephropathy. hyperkalemia. ATII increases blood pressure using a number of mechanisms. ADH stimulates further water reabsorption from the kidneys via insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules. particularly thiazide diuretics). The potential for symptomatic hypotension with ACE inhibitor therapy requires careful monitoring. ATII stimulates the secretion of vasopressin (also known as antidiuretic hormone or ADH) from the posterior pituitary gland. water and electrolyte balance. Aldosterone travels to the distal convoluted tubule (DCT) and collecting tubule of nephrons where it increases sodium and water reabsorption by increasing the number of sodium channels and sodium-potassium ATPases on cell membranes. competes with ATI (Angiotensin) for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII.g. tab 50 mg Nr. During sympathetic stimulation or when renal blood pressure or blood flow is reduced. Third. c) Pharmacologic effects: Captopril. angioedema. May be used to treat congestive heart failure in combination with other drugs (e. g) Pharmacography: Tablets: 12. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII. antagonizes the effect of the RAAS. and a persistent dry cough. ACE inhibitors inhibit the rapid conversion of ATI to ATII and antagonize RAASinduced increases in blood pressure. 1 tabl/day for 30 days . Orally. First. cardiac glycosides. an ACE inhibitor. renin is released from the granular cells of the juxtaglomerular apparatus in the kidneys. which is subsequently cleaved to ATII by ACE. Captopril’s affinity for ACE is approximately 30. In the blood stream. e) Adverse effects: These include postural hypotension. β-adrenergic blockers). Second.000 times greater than that of ATI. it stimulates the secretion of aldosterone from the adrenal cortex. renal insufficiency. In addition to these major effects.s.5mg – 25mg – 50mg – 100mg h) Prescription : Dg/Hypertension Rp/Captopril. ATII induces the thirst response via stimulation of hypothalamic neurons. Stimulation of the Type 1 ATII receptor on vascular smooth muscle cells leads to a cascade of events resulting in myocyte contraction and vasoconstriction.{ PHYSIOLOGY : The RAAS is a homeostatic mechanism for regulating hemodynamics. May improve survival in patients with left ventricular dysfunction following myocardial infarction. because they are fetotoxic.XXX D. including diabetic nephropathy.a) Pharmacological class: Angiotensin-converting enzyme (ACE) b) Mechanism of action: Captopril. Captopril also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors. one of the few ACE inhibitors that is not a prodrug. ACE (also known as kininase II) is also involved in the enzymatic deactivation of bradykinin. diuretics. a vasodilator. ATII increases blood pressure through direct arterial vasoconstriction. Anaphylactoid reaction is plausible. f) Contraindications: ACE inhibitors should not be used in pregnant women.

Orally. 80 mg. c) Pharmacologic effects: All the ARBs are approved for treatment of hypertension based on their clinical efficacy in lowering blood pressure and reducing the morbidity and mortality associated with hypertension. d) Therapeutic uses: May be used as a first line agent to treat uncomplicated hypertension. Their use in HF is as a substitute for ACE inhibitors in those patients with severe cough or angioedema.a) Pharmacological class: Angiotensin II-receptor blocker (ARB) b) Mechanism of action: Valsartan is an ARB that selectively inhibits the binding of angiotensin II to AT I. Usual dosage from 40–320 mg daily. Losartan may be also used as a second line agent in the treatment of congestive heart failure. Tablets combined with diuretics: (valsartan/HCTZ mg) 80 or 160 or 320/12. myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors. because they are fetotoxic. tab 160 mg Nr. 80 mg.5 mg and 160 or 320/25 mg. e) Adverse effects: Headache and dizziness and sometimes fatigue. which is found in many tissues such as vascular smooth muscle and the adrenal glands.XXX D. g) Pharmacography: Caps: 40 mg. May be used as a first line agent to delay progression of diabetic nephropathy. systolic dysfunction. 160 mg. This effectively inhibits the ATI-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Inhibition of aldosterone secretion may inhibit sodium and water reabsorption in the kidneys while decreasing potassium excretion. h) Prescription : Dg/Hypertension Rp/Valsartanl. isolated systolic hypertension and left ventricular hypertrophy. f) Contraindications: ACE inhibitors should not be used in pregnant women. or 160 mg Tablets: 40 mg .s. Valsartan is selective for AT and has virtually no affinity for ATII. 1 tab/day for 30 days . or 320 mg.