Pr Dr Agit Diare.docx

Indications

Codeine

Dosage

Adult : PO Pain 15-60 mg 4 hrly. Max: 360 mg/day. Cough suppressant 15-30 mg 3-4 times daily.Acute diarrhoea 15-60 mg 3-4 times daily. Syr 1-2 5 mL every 4-6 hr. IV/IM/SC Pain30-60 mg 4 hrly. Max: 240 mg/day.

Dosage Details

Oral Acute diarrhoea Adult: 15-60 mg 3-4 times daily. Oral Mild to moderate pain Adult: 15-60 mg 4 hrly. Max: 360 mg/day. Child: ≤12 yr 0.5-1 mg/kg every 4-6 hr daily. Max: 240 mg daily. Oral Cough suppressant Adult: 15-30 mg 3-4 times daily. Child: 2-5 yr 3 mg; 6-12 yr 7.5-15 mg. Doses to be taken 3-4 times daily. Parenteral Mild to moderate pain Adult: IV/IM/SC: 30-60 mg 4 hrly. Max: 240 mg/day.

Renal Impairment

Dose adjustment may be needed.

Hepatic Impairment

Dose adjustment may be needed.

Administration

May be taken with or without food.

Contraindications

Respiratory depression; obstructive airway disease; acute and severe asthma attack; presence or suspicion of paralytic ileus, acute ulcerative colitis, antibiotic-associated colitis; comatose patients; acute alcoholism. Patients w/ head injury, raised intracranial pressure. Use in childn after tonsillectomy and/or adenoidectomy. Coadministration w/ MAO inhibitors or w/in 2 wk of its discontinuation. Childn <1 yr.

Special Precautions

Hypothyroidism, adrenocortical insufficiency; prostatic hyperplasia, hypotension, shock, inflammatory or obstructive bowel disorders, myasthenia gravis. Patient who are ultra-rapid metabolisers of codeine. Renal and hepatic impairment. Pregnancy and lactation. Elderly or debilitated patients.

Adverse Drug Reactions

Dependence, withdrawal symptoms; nausea, vomiting, constipation, drowsiness, confusion, difficulty in micturition, ureteric or biliary spasms, urinary retention, dry mouth, dizziness, sweating, facial flushing, headache, vertigo, bradycardia, tachycardia, palpitations, oedema, postural hypotension, hypothermia, vertigo, restlessness, mood changes, decreased libido or potency, hallucination, miosis, raised intracranial pressure, muscle rigidity, visual disturbances. Potentially Fatal: Respiratory depression and hypotension, w/ circulatory failure and deepening coma (larger doses). Convulsions (especially in childn and infants). Rhabdomyolysis.

Pregnancy Category (US FDA)

Parenteral/PO: C, D (if prolonged use/high doses at term)

Patient Counselling

May impair ability to drive or operate machinery.

Monitoring

Monitor BP, heart rate, respiratory and mental status.

Parameters Overdosage

Symptoms: Somnolence, rash, miosis, vomiting, itching, ataxia, skin swelling, CNS depression, respiratory depression, pinpoint-sized pupil. Management: Symptomatic and supportive treatment including airway clearing and monitoring vital signs. Emptying the stomach by aspiration or lavage. If ingestion of >350 mg by an adult or >5 mg/kg by a child occur w/in an hour, consider activated charcoal. Administer naloxone in cases of coma or respiratory depression, observe for at least 4 hr after ingestion.

Drug Interactions

Enhanced depressant effects w/ anaesthetics, anxiolytics, hypnotics, TCAs, antipsychotics. May alter effects of other compounds e.g. mexiletine, metoclopramide and domperidone. Potentially Fatal: Additive effects w/ MAOI, avoid combination.

Food Interaction

Additive depressant effects w/ alcohol. Avoid use w/ valerian, St John's wort, kava kava and gotu kola as it may increase CNS depression.

Mechanism of Action

Description: Codeine is a phenantrene-derivative opiate agonist which alters the perception of and response to pain by binding to opiate receptors in the CNS, blocking the ascending pain pathways. It also helps suppress cough by direct action in the medulla. Onset: Oral: 0.5-1 hr. Duration: 4-6 hr. Pharmacokinetics: Absorption: Adequate absorption in GI tract. Time to peak plasma concentration: 1-1.5 hr. Distribution: Crosses placenta and enters breast milk. Plasma protein binding: Approx 725%. Volume of distribution: Approx 3-6 L/kg. Metabolism: Hepatic by O- and N-demethylation to morphine (active), norcodeine and other metabolites including normorphine and hydrocodone. Excretion: Via urine, mainly as conjugates w/ glucuronic acid. Plasma half-life: About 3-4 hr.

Storage

Store between 15-30°C.

MIMS Class

Cough & Cold Preparations / Analgesics (Opioid)

In treating diarrhoea, codeine works by acting on opioid receptors that are found in the muscles lining the walls of the intestines. This reduces the muscular contractions of the intestine (called peristalsis) that move food and faecal matter through the gut. The speed at which the gut contents are pushed through the intestines is therefore reduced, allowing more time for water and electrolytes to be reabsorbed from the gut contents back into the body. This results in firmer stools that are passed less frequently.

ndications

Loperamide

Dosage

Adult : PO Acute diarrhoea Initial: 4 mg, then 2 mg after each loose stool. Max: 16

mg/day. Chronic diarrhoea Initial: 4-8 mg/day in divided doses. Max: 16 mg/day. Dosage Details

Oral Acute diarrhoea Adult: Initially, 4 mg followed by 2 mg after each loose stool. Max: 16 mg daily. Discontinue if clinical improvement is not observed w/in 48 hr. Child: 4-8 yr 1 mg 3-4 times daily for up to 3 days; 9-12 yr 2 mg 4 times daily for up to 5 days. Oral Chronic diarrhoea Adult: Initially, 4-8 mg daily in divided doses, adjusted if necessary. Max: 16 mg daily; discontinue if no improvement at this dose after 10 days.

Administration

May be taken with or without food.

Contraindications

Conditions when inhibition of peristalsis is to be avoided; antibiotic-associated colitis, acute ulcerative colitis, bacterial enterocolitis, acute inflammatory bowel disease, abdominal distention.

Special Precautions

Not intended for use as a primary treatment in acute dysentery. Hepatic impairment. Childn. Pregnancy and lactation.

Adverse Drug Reactions

Abdominal pain or bloating, nausea and vomiting, constipation, dry mouth, drowsiness, dizziness, fatigue, epigastric pain, hypersensitivity reactions (e.g. rash). Potentially Fatal: Paralytic ileus (particularly in infants and young childn).

Pregnancy Category (US FDA)

ROUTE(S) : PO

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1sttrimester (and there is no evidence of a risk in later trimesters). Patient Counselling Monitoring Parameters

This drug may cause drowsiness or dizziness, if affected it may impair ability to drive or operate machinery. Monitor for signs of CNS toxicity (in patients w/ hepatic impairment).

Overdosage

Symptoms: CNS depression; constipation, urinary retention and ileus may occur. Management: Employ gastric lavage followed by admin of activated charcoal. Naloxone HCl may be given as antidote.

Drug Interactions

Increased plasma levels w/ P-glycoprotein inhibitors (e.g. quinidine, ritonavir). May decrease exposure to saquinavir.

Mechanism of Action

Description: Loperamide reduces propulsive peristalsis and increases intestinal transit by binding to the opiate receptor in the gut wall. It also increases the tone of the anal sphincter, thereby reducing incontinence and urgency. Pharmacokinetics: Absorption: Approx 40% is absorbed from the GI tract. Time to peak plasma concentration: 2.5 hr (oral soln); 5 hr (cap). Metabolism: Hepatically converted to desmethylloperamide via N-demethylation by CYP2C8 and CYP3A4 isoenzymes, CYP2B6 and CYP2D6 also play a role. Excretion: Via faeces (as inactive conjugate); urine. Elimination half-life: Approx 10 hr.

Storage

Store between 20-25°C.

MIMS Class

Antidiarrheals

ATC Classification

A07DA03 - loperamide ; Belongs to the class of antipropulsives. Used in the treatment of diarrhea.

Manufacturer

Sandoz

Contents

Colloidal activated attapulgite

Indications

Symptomatic treatment of nonspecific diarrhoea.

Dosage

Adult 2 tab after initial bowel movement & 2 tab after subsequent bowel movement. Max daily dose: 12 tab. Childn 6-12 yr ½ adult dose. Max daily dose: 6 tab.

Administration

May be taken with or without food.

Contraindications

GIT stenotic lesions. Presence of high fever.

Special Precautions

Therapy should not be exceeded >2 days or in the presence of fever. Childn <6 yr. Severe renal insufficiency.

Drug Interactions

May influence GI absorption of tetracyclines.

MIMS Class

Antidiarrheals

ATC Classification

A07BC04 - attapulgite ; Belongs to the class of other intestinal adsorbents.

Drug Classification

B

Presentation/Packing

Form Biodiar tab 630 mg

Packing/Price 25 × 4's (Rp103,000/boks) 5 × 10's (Rp61,800/boks)

Indications

Active charcoal

Dosage

Adult : PO Acute oral poisoning 25-100 g as a single dose. GI disorders 0.975-3.9 g 3 times/day.

Dosage Details

Oral Acute oral poisoning Adult: 25-100 g as a single dose. For multiple-dose treatment: 50-100 g as an initial dose followed by not <12.5 g every hr. Alternatively, 25 mg every 2 hr or 50 mg every 4 hr. Child: <1 yr: 1 g/kg/dose; 1-12 yr: 25-50 g/dose. Oral

Gastrointestinal disorders Adult: 0.975 - 3.9 g tid. Contraindications

Cyanide, mineral acids, caustic alkalis, organic solvents, iron, ethanol, methanol poisoning; lithium, methionine; intestinal obstruction, anatomically-broken GI tract, haemorrhage or GI perforation. Concomitant use of charcoal with sorbitol: Patients with fructose intolerance; Childn <1 yr.

Special Precautions

Decreased peristalsis: administer within 1 hr of ingestion. Induce vomiting of ipecac syr before admin of charcoal to prevent adsorption of ipecac. Petroleum distillate, caustic ingestions may harm gastric lining upon induction of vomiting by charcoal. Limit admin of charcoal in sorbitol doses to prevent loss of fluid and electrolyte. Monitor for active bowel sounds before administering charcoal. Pregnancy.

Adverse Drug Reactions

Vomiting, constipation, diarrhoea, black stools, swelling of abdomen, bowel obstruction; platelet aggregation, charcoal embolism, thrombocytopenia, haemorrhage, hypoglycaemia, hypocalcaemia, hypothermia, hypotension (haemoperfusion with activated charcoal); blackening of teeth and mouth; hypernatraemia, hypokalaemia, hypermagnesemia (with concomitant admin with cathartics).

Drug Interactions

Reduces absorption of most drugs from GI tract. Decreases effectiveness of methionine via adsorption. Decreases ipecac effect.

Food Interaction

Milk products eg, milk, ice crm or sherbet, marmalade reduces charcoal effect. Food, nutritional supplements or herbs must not be taken within two hr of ingestion of charcoal.

Mechanism of Action

Description: Charcoal due to its large surface area, inhibits the GI absorption of toxic substances or irritants eg, aromatic or benzenoid-type substances through adsorption. As a laxative, the addition of sorbitol provides hyperosmotic environment thus causing catharsis. Moreover, charcoal interferes with the enterohepatic circulation of bile acids resulting to a lower cholesterol level. Pharmacokinetics: Absorption: Unabsorbed via the GI tract. Metabolism: Unmetabolised. Excretion: Via faeces (as unchanged form).

MIMS Class

Antidotes & Detoxifying Agents

Manufacturer

Sanbe

Contents

Chlordiazepoxide 5 mg, clidinium Br 2.5 mg

Indications

Autonomic & somatic symptoms because of anxiety. Symptomatic treatment of peptic ulcer, hypersecretory & hypermotility of GIT, nervous dyspepsia, spastic & irritable colon, biliary, dyskinesia, ureter spasm & ureter dyskinesia, irritable bowel syndrome, colitis, diarrhoea, dysmenorrhoea.

Dosage

Adult 3-4 tab daily. Elderly & debilitated Initially 1-2 tab daily, increase gradually to the effective dose.

Administration

Should be taken on an empty stomach: Take before meals & bedtime.

Contraindications

Prostatic hypertrophy & glaucoma.

Special Precautions

Hepatic disorder, long-term therapy. Pregnancy (1st trimester).

Adverse Drug Reactions

Mental & visual disturbance, drowsiness, amnesia, dependence; urinary retention, hypotension.

View ADR Monitoring Form Drug Interactions

Cimetidine; alcohol, other CNS depressants.

MIMS Class

Antispasmodics

ATC Classification

A03CA02 - clidinium and psycholeptics ; Belongs to the class of synthetic anticholinergic antispasmodics, in combination with psycholeptics. Used in the treatment of functional gastrointestinal disorders.

Drug Classification

G

Presentation/Packing

Form Braxidin FC tab

Packing/Price 10 × 10's (Rp80,000/boks)

Chlordiazepoxide hydrochloride and clidinium bromide (Librax) combines the anti-anxiety action of chlordiazepoxide and the antispasmodic effects of clidinium. It also blocks the acid secretion of the gastrointestinal tract and inhibits the action of nerves that are very active in certain diseases. The FDA classifies the combination as possibly effective as additional therapy for treatment of peptic ulcers, irritable bowel syndrome (IBS), GI spasms and some intestinal infections. ndications

Listed in Dosage.

Dosage

Adult : PO Heart failure; Supraventricular arrhythmias Rapid digitalisation: Loading dose: 0.75-1.5 mg in the 1st 24 hr. Slow digitilisation: 250 mcg 1-2 times/day. Uusal maintenance: 125-250 mcg/day.IV Emergency heart failure For patients who have not received cardiac glycosides in the previous 2 wk: 0.5-1 mg via infusion as a single dose or in divided doses. Maintenance: Usually via oral admin.

Dosage Details

Intravenous Emergency treatment in heart failure Adult: For patients who have not received cardiac glycosides in the previous 2 wk. 0.5-1 mg by IV infusion as a single dose over at least 2 hr or in divided doses with each dose given over 10-20 minutes. Maintenance dose is usually given orally. Oral Heart failure, Supraventricular arrhythmias Adult: Rapid digitalisation: Loading dose of 0.75-1.5 mg during the first 24-hr period as a single dose or in divided doses every 6 hr for less urgent or greater risk cases. For mild heart failure: Loading dose may not be required, 250 mcg 1-2 times daily. For patients with normal renal function, steady-state plasma concentrations are usually achieved in about 7 days. Usual maintenance: 125-250 mcg daily but may range from 62.5-500 mcg daily. Child: Neonate <1.5 kg: Initial: 25 mcg/kg/day in 3 divided doses for 24 hr, then 4-6 mcg/kg/day in 1-2 divided doses; neonate 1.5-2.5 kg: Initial: 30 mcg/kg/day in 3 divided doses for 24 hr, then 4-6 mcg/kg/day in 1-2 divided doses; Neonate >2.5 kg and child 1 mth2 yr: Initial: 45 mcg/kg/day in 3 divided doses for 24 hr, then 10 mcg/kg/day in 1-2 divided doses. 2-5 yr: Initial: 35 mcg/kg/day in 3 divided doses for 24 hr, then 10 mcg/kg/day in 1-2 divided doses. 5-10 yr: Initial: 25 mcg/kg/day (max: 750 mcg/day) in 3 divided doses for 24 hr, then 6 mcg/kg/day (max: 250 mcg/day) in 1-2 divided doses. 10-18 yr: Initial: 0.75-1.5 mg/day in 3 divided doses for 24 hr, then 62.5-750 mcg/day in 1-2 divided doses. Reduce doses if patient has been given cardiac glycoside in the preceding 2 wk. Elderly: Lower doses are given.

Renal Impairment

Dosage reductions may be needed.

Administration

May be taken with or without food.

Reconstitution

Intravenous: Admin undiluted or diluted with a 4-fold or greater volume of sterile water for inj, NaCl 0.9% inj, or dextrose 5% inj.

Incompatibility

Using less than a 4-fold volume of diluent could lead to precipitation of the digoxin.

Contraindications

Digitalis toxicity, ventricular tachycardia/fibrillation, obstructive cardiomyopathy. Arrhythmias due to accessory pathways (e.g. Wolff-Parkinson-White syndrome).

Special Precautions

Cardiac dysrhythmias, hypokalaemia, hypertension, IHD, hypercalcaemia, hypomagnesaemia, electroconversion, chronic cor pulmonale, aortic valve disease, acute myocarditis, congestive cardiomyopathies, constrictive pericarditis, heart block, elderly, renal impairment, abnormalities in thyroid function; pregnancy. IV digoxin can only be given to patients who have not received cardiac glycosides in the preceding 2 wk.

Adverse Drug Reactions

Extra beats, anorexia, nausea and vomiting. Diarrhoea in elderly, confusion, dizziness, drowsiness, restlessness, nervousness, agitation and amnesia, visual disturbances, gynaecomastia, local irritation (IM/SC inj), rapid IV admin may lead to vasocostriction and transient hypertension. Potentially Fatal: Cardiac arrhythmias in combination with heart block.

Pregnancy Category (US FDA)

ROUTE(S) : Parenteral/PO

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. Overdosage

Symptoms: Hyperkalaemia, cardiac arrhythmias and heart block. Management: Treatment is symptomatic and supportive. Reduce absorption by gastric lavage if present within 30 min of ingestion. Do not induce vomiting or attempt passage of a gastric tube if presented >2 hr after ingestion or already has toxic manifestations, as this may induce an acute vagal episode and worsen digitalis-related arrhythmias. Activated charcoal is helpful in reducing drug absorption. Monitor serum potassium levels and keep potassium levels between 4.0-5.5 mmol/l. Digoxin-specific antibody fragments (FAB) is a specific antidote for digoxin and may be used to reverse potentially life-threatening ventricular arrhythmias due to digoxin overdosage. Haemodialysis is unlikely to be useful.

Drug Interactions

Effectiveness reduced by phenytoin, neomycin, sulphasalazine, kaolin, pectin, antacids and in patients receiving radiotherapy. Metoclopramide may alter the absorption of solid dosage forms of digoxin. Blood levels increased by calcium channel blockers, spironolactone, quinidine and calcium salts. Potentially Fatal: Electrolyte imbalances such as hypokalaemia and hypomagnesemia (e.g. admin of potassium-losing diuretics, corticosteroids) can increase the risk of cardiac toxicity.

Food Interaction

Absorption delayed.

Lab Interference

May increase conc of urinary 17-hydroxycorticosteroids.

Mechanism of Action

Description: Digoxin is a cardiac glycoside which has positive inotropic activity characterized by an increase in the force of myocardial contraction. It also reduces the conductivity of the heart through the atrioventricular (AV) node. Digoxin also exerts direct action on vascular

smooth muscle and indirect effects mediated primarily by the autonomic nervous system and an increase in vagal activity. Pharmacokinetics: Absorption: Absorption from the GI tract is variable. Distribution: Widely distributed in tissues, including the heart, brain, erythrocytes, and skeletal muscle. 20-30% bound to plasma proteins. Excretion: Excreted mainly unchanged. Storage

Store at 25°C.

MIMS Class

Cardiac Drugs

Laxadyn

Lactulax

Dulcolax