anasthetic drugs

7/29/2019 Anasthetic Drugs

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NOREPINEPHRINE

Indication & Dosage Intravenous

Acute hypotensive states

Adult: Initially, 8-12 mcg/minute, up to 8-30 mcg/minute in refractoryshock. Infuse using a

solution of 4 mcg/ml in glucose 5%, or sodium chloride 0.9% and glucose 5% at a rate of 2-3

ml/minute. Adjust according to BP response. Average maintenance dose: 0.5-1 ml/minute (2-

4 mcg/minute). Infuse via a central venous catheter or into a large vein.

Child:Administer at a rate of 2 mcg/minute. Alternatively, 2 mcg/m2/minute. Adjust rate

according to BP response and perfusion.

Elderly: Initial dose should be at low end of dose range.

Injection

Upper gastrointestinalhaemorrhage

Adult: Intraperitoneal admin: 8 mg in 250 ml of 0.9% sodium chloride inj. Alternatively, instill

8 mg in 100 ml of 0.9% sodium chloride solution through a nasogastric tube every hr for 68

hr, then every 2 hr for 46 hr. Withdraw drug gradually.

Reconstitution: Dilute with 5% glucose inj, with or without sodium chloride; dilution withsodium chloride inj alone is not recommended.

Incompatibility: Incompatible with alkali and oxidising agents, barbiturates, chlorphenamine,

chlorothiazide, nitrofurantoin, novobiocin, phenytoin, sodium bicarbonate, sodium iodide,

streptomycin, insulin.

Overdosage Symptoms: Hypertension, sweating, cerebral haemorrhage, convulsions.

Contraindications Hypertension. Pregnancy. Patients with peripheral or mesenteric vascular thrombosis unless

necessary as a life-saving procedure.

Special Precautions Not a substitute for replacement of blood, plasma, fluids, and/or electrolytes; correct volume

depletion prior to admin. Identify and correct hypoxia, hypercapnia and acidosis prior to or

during admin. Avoid extravasation as tissue necrosis may occur. Avoid inj into leg veins,especially in elderly or those with occlusive vascular diseases, arteriosclerosis, DM or

Buerger's disease. Hypertensive or hyperthyroid patients. In conjunction with local

anaesthetics, do not use in fingers, toes, ears, nose or genitalia. Lactation.

Adverse Drug

Reactions

Hypertension, headache, peripheral ischaemia, bradycardia, arrhythmias, anxiety, skin

necrosis (with extravasation), dyspnoea, respiratory difficulty.

Drug Interactions Guanethidine, methyldopa,reserpine, TCAs may increase pressor response to

norepinephrine.

Potentially Fatal: Increased risk of arrhythmias with cocaine, cyclopropane or halogenated

hydrocarbon anaesthetics. Hypertensive crisis may occur with MAOIs. Hypertensive effects

may be increased by nonselective -blockers.

Click to view more norepinephrine Drug Interactions

Pregnancy Category

(US FDA)

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.
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Storage Intravenous: Store at room temperature (25C) and protect from light. Store in tight, light-

resistant containers as norepinephrine is readily oxidised. Do not use if discoloured (e.g.

pink, dark yellow, brown) or if there is a precipitate.

Mechanism of Action Norepinephrine is a direct-acting sympathomimetic which stimulates 1- and -adrenergic

receptors. Its -agonist effects cause vasoconstriction, thereby raising systolic and diastolic

BP with reflex slowing of heart rate.

Onset: Rapid.

Duration: Short; stops within 1-2 min after discontinuing the infusion.

Absorption: Oral: Destroyed in the GI tract; SC: Poorly absorbed.

Distribution: Mainly localises in sympathetic nervous tissue; crosses the placenta but not the

blood-brain barrier.

Metabolism: Metabolised in the liver and in other tissues by the enzymes catechol-O-

methyltransferase (COMT) and monoamine oxidase (MAO).

Excretion: Via urine (mainly as metabolites).

MIMS Class Vasoconstrictors

ATC Classification C01CA03 - norepinephrine ; Belongs to the class of adrenergic and dopaminergic cardiac

stimulants excluding glycosides. Used in the treatment of heart failure.
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EPINEPHRINE

Indication & Dosage Inhalation

Acuteasthma

Adult: Spray: Aqueous solution with anadrenalinecontent equivalent to 1:100. Pressurised

aerosols delivering metered doses equivalent to approximately 160-275 mcg: 1-2 inhalations,

may repeat after 3 hr if necessary.

Parenteral

Acuteasthma

Adult:As 1:1,000 aqueous solution: 0.3-0.5 ml (300-500 mcg). Dose may be given via IM or

SC inj.

Child:As 1:1,000 aqueous solution: 0.01 ml/kg (10 mcg/kg). Max: 0.5 ml (500 mcg). Dose

may be given via IM or SC inj.

Intravenous

Advanced cardiac life support

Adult: Initially, 1 mg (10 mL of a 1:10,000 solution), may repeat as often as every 2-3

minutes throughout the resuscitation process. May also be given via intraosseous route at

the same dosage. For endotracheal doses: 2-3 times of the IV dose.Child: Initially, 10 mcg/kg, may repeat as often as every 2-3 minutes throughout the

resuscitation process. Endotracheal doses: 100 mcg/kg. Intraosseous doses are the same as

IV doses.

Max Dosage: Intraosseous doses for adults and children are the same as IV doses.

Intravenous

Anaphylactic shock

Adult: 0.5 mg (5 mL of a 1:10,000 solution) given at a slow rate of 100 mcg/minute, stopping

when a response is achieved.

Child: 10 mcg/kg. If autoinjectors are used, doses are based on body wt: 15-30 kg: 150 mcg

and >30 kg: 300 mcg.

IntramuscularAnaphylactic shock

Adult:As 1:1,000 solution: 500 mcg (0.5 ml), repeat every 5 minutes as needed until

improvement occurs. For emergency self-admin (e.g. via autoinjector): A dose of 300 mcg

(0.3 ml) may be used.

Child: Dose depends on age and weight. Usual dose: 10 mcg/kg.

Ophthalmic

Ocular hypertension

Adult: Instill 0.5%, 1% or 2% eye drops once or twice daily.

Ophthalmic

Open-angle glaucoma

Adult: Instill 0.5%, 1% or 2% eye drops once or twice daily.

Overdosage Overdosage intravascular inj of epinephrine may cause cerebral haemorrhage due to a sharp

rise in BP. Fatalities may also result from pulmonary oedema because of peripheral vascular

constriction together with cardiac stimulation.

Contraindications Preexisting hypertension; occlusive vascular disease; angle-closure glaucoma (eye drops);

hypersensitivity; cardiac arrhythmias or tachycardia. When used in addition to local

anaesthetics: Procedures involving digits, ears, nose, penis or scrotum.

Special Precautions CV diseases; hyperthyroidism; DM; Parkinson's disease; elderly; pregnancy, lactation.
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Adverse Drug

Reactions

CNS effects; GI disturbances; epigastric pain; CV disorders; difficulty in micturition with

urinary retention; dyspnoea; hyperglycaemia; sweating; hypersalivation; weakness, tremors;

coldness of extremities; hypokalaemia. Gangrene, tissue necrosis and sloughing

(extravasation) when used in addition to local anaesthetics. Eye drops: Severe smarting,

blurred vision, photophobia; naso-lachrymal ducts obstruction. Oedema, hyperaemia and

inflammation of the eyes with repeated administration.

Drug Interactions Halogenated inhalation anaesthetics; - or -blocking agents; methyldopa,guanethidine;

drugs with vasoconstrictor and pressor effects; antihypertensives; adrenergic neuron

blockers; potassium-depleting drugs; cardiac glycosides; ephedra, yohimbe. TCAs may

induce hypertension and arrhythmia.

Click to view more epinephrine Drug Interactions

Lab Interference Increase in bilirubin, catecholamines, glucose, uric acid.

Pregnancy Category

(US FDA)





Storage Inhalation: Store at 25C. Intramuscular: Store at 25C. Intravenous: Store at

25C. Ophthalmic: Store at 25C.Parenteral: Store at 25C.

Mechanism of Action Epinephrine, an active principle of the adrenal medulla, is a direct-acting sympathomimetic. It

stimulates - and -adrenergic receptors resulting in relaxation of smooth muscle of the

bronchial tree, cardiac stimulation and dilation of skeletal muscle vasculature. It is frequently

added to local anaesthetics to retard diffusion and limit absorption, to prolong the duration of

effect and to lessen the danger of toxicity.

Onset: SC: approx 5-10 min; inhalation: approx 1 min; conjunctival instillation: IOP declines

approx 1 hr.Duration: Ocular effect: 12-24 hrs.

MIMS Class Cardiac Drugs/Antiasthmatic & COPD Preparations/Antiglaucoma Preparations

ATC Classification A01AD01 - epinephrine ; Belongs to the class of other agents for local oral treatment.

S01EA01 - epinephrine ; Belongs to the class of sympathomimetics used in the treatment of

glaucoma.

C01CA24 - epinephrine ; Belongs to the class of adrenergic and dopaminergic cardiac


R01AA14 - epinephrine ; Belongs to the class of topical sympathomimetic agents used as

nasal decongestants.

B02BC09 - epinephrine ; Belongs to the class of local hemostatics. Used in the treatment of

hemorrhage.

R03AA01 - epinephrine ; Belongs to the class of adrenergic inhalants, alpha- and beta-

adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.
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DOPAMINE


Acuteheart failure

Adult:As hydrochloride: Initially, 1-5 mcg/kg/min increased gradually by up to 5-10

mcg/kg/min according to the patient's BP, cardiac output and urine output. Up to 20-50

mcg/kg/min may be required in seriously ill patients.

Overdosage Symptoms include excessive BP elevation. Treatment includes reducing rate of admin or

temporarily discontinuing therapy until patient's condition stabilises. Usually, no additional

remedial measures are needed as dopamine has short duration of action. In severe cases,

short-acting -adrenergic blocking agent, phentolamine, may be used.

Contraindications Pheochromocytoma, uncorrected tachyarrhythmias, ventricular fibrillation. Hypersensitivity.

Special Precautions Shock secondary to MI, history of peripheral vascular disease. Correct hypovolaemia before

infusion. History of occlusive vascular disease e.g, atherosclerosis, Raynaud's disease,

Buerger's disease, diabetic endarteritis; disproportionate increase in diastolic pressure.

Pregnancy.

Adverse Drug

Reactions

Nausea, vomiting, tachycardia, ectopic beats, palpitation, anginal pain, hypotension,

vasoconstriction, bradycardia, hypertension, dyspnoea, headache, widened QRS complexes,

azotaemia.

Drug Interactions Cyclopropane and halogenated hydrocarbon anaesthetics may sensitise myocardium to

dopamine and precipitate ventricular arrhythmias. MAO inhibitors prolong and increase

dopamine effects. Ergots potentiate vasoconstriction action of dopamine. Alpha-blockers

unmask dopamine's beta action.

Click to view more dopamine Drug Interactions

Lab Interference Suppresses pituitary secretion of thyroid-stimulating hormone, growth hormone and prolactin.

Pregnancy Category

(US FDA)





Storage Intravenous: Store below 30C.

Mechanism of Action Dopamine stimulates dopaminergic receptors at lower doses producing renal and mesenteric

vasodilation while at higher doses stimulate both dopaminergic and -adrenergic receptors

producing cardiac stimulation and renal vasodilation. It increases heart rate and force of

contraction. At low infusion rates vasodilatation occurs in the renal, mesenteric, coronary and

cerebral beds. At higher rates vasoconstriction in skeletal muscles and a rise in BP.Absorption: Inactivated in the GI tract and body (oral).

Metabolism: Into dopamine-related products; converted to noradrenaline.

Excretion: Eliminated as metabolic products of noradrenaline; 2 min (elimination half-life).

MIMS Class Cardiac Drugs

ATC Classification C01CA04 - dopamine ; Belongs to the class of adrenergic and dopaminergic cardiac

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PHENYLEPHRINE

Indication & Dosage Oral

Nasal congestion

Adult:As hydrochloride: 10 mg every 4 hr, max 60 mg daily; or 12 mg up to 4 times daily.

Child: Child: 2-6 yr: As tannate salt: 1.87-3.75 mg every 12 hr. 6-12 yr: As hydrochloride salt:

10 mg every 4 hr; as tannate salt: 3.75-7.5 mg every 12 hr. >12 yr: As hydrochloride salt: 10-

20 mg every 4 hr; as tannate salt: 7.5-15 mg every 12 hr.

Nasal

Nasal congestion

Adult: 0.25 to 1% solution: Instill as nasal drops or a spray into each nostril every 4 hr as

needed.

Child: 2-6 yr: 0.125% or 0.16% solution: 2-3 drops into each nostril every 4 hr as needed; 6-

12 yr: 0.25% solution: 2-3 drops, or 1-2 sprays, into each nostril every 4 hr as needed.

Parenteral

Hypotensive states

Adult:As hydrochloride: Hypotension: Initially, 2-5 mg as a 1% solution via SC/IM admin

with further doses of 1-10 mg if necessary; or 100-500 mcg by slow IV inj as a 0.1% solution,repeat as necessary after at least 15 min. Severe hypotension: 10 mg in 500 ml of glucose

5% or sodium chloride 0.9% infused IV at initial rate of up to 180 mcg/min reduce to 30-60

mcg/min according to response.

Child:Acute hypotension: Subcutaneous/IM: 1-12 yr: 100 mcg/kg every 1-2 hr as needed

(max: 5 mg); 12-18 yr: 2-5 mg, followed by further doses of 1-10 mg (max initial dose 5 mg) if

necessary. IV injection: 1-12 yr: 5 to 20 mcg/kg (max 500 mcg), repeated as needed after at

least 15 min; 12-18 yr: 100-500 mcg, repeated as needed after at least 15 min. IV infusion:

Solution is diluted with glucose 5% or sodium chloride 0.9% to a concentration of 20 mcg/ml

and given via a central venous catheter. 1-16 yr: 100-500 nanograms/kg/min, adjusted

according to response; 16-18 yr: initially up to 180 mcg/min, reduced to 30-60 mcg/min

according to response.Injection

Paroxysmal supraventricular tachycardia

Adult:As hydrochloride: Initially, max of 500 mcg as a 0.1% solution, subsequent doses

gradually increase by 100-200 mcg, up to 1 mg, if necessary.

Ophthalmic

Mydriasis

Adult:As hydrochloride: Up to 10%. Instill 1 drop, may repeat in 10-60 minutes as needed.

May cause intense irritation and a local anaesthetic other than butacaine (incompatible)

should be instilled into the eye a few minutes beforehand.

Child: 2.5% solution: 72 hr.

Rectal

Haemorrhoids

Adult: Cream/ointment: Apply to clean dry area, up to 4 times daily; may be used externally

or inserted rectally using applicator. Suppository: Insert 1 suppository, up to 4 times daily.
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Child: 12 yr: Cream/ointment: Apply to clean dry area, up to 4 times daily; may be used

externally or inserted rectally using applicator. Suppository: Insert 1 suppository, up to 4

times daily.

Administration Should be taken with food.

Overdosage Vomiting, hypertension, palpitations, paresthesia, ventricular extrasystoles. Treatment is

supportive; in extreme cases, IV phentolamine may be used.

Contraindications Hypertension, ventricular tachycardia. Oral: use with or within 14 days of MAOI therapy.

Ophthalmic: narrow-angle glaucoma.

Special Precautions Severe hyperthyroidism, severe ischaemic heart disease, DM, prostatic hyperplasia.

Rebound congestion in prolonged or excessive use of nasal drops. Use 10% eye drops in

extreme caution in infants, elderly, cardiac disease, significant hypertension, advanced

arteriosclerosis. Pregnancy and lactation. Over-the-counter cough and cold medications

should not be used in infants and children


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Duration: Subcutaneous: 1 hr; IM: Up to about 2 hr; IV: 15-30 min; Ophthalmic: maximal

mydriasis: 1 hr, recover time: 3-6 hr.

Absorption: Systemic absorption follows topical application.

Metabolism: Via intestinal monoamine oxidase to phenolic conjugates in the liver.

Excretion: Via urine (90%).

MIMS Class Mydriatic Drugs/Cough & Cold Preparations/Nasal Decongestants & Other Nasal

Preparations/Ophthalmic Decongestants, Anesthetics, Anti-

Inflammatories/Vasoconstrictors/Anorectal Preparations

ATC Classification R01AB01 - phenylephrine ; Belongs to the class of topical sympathomimetic combination

preparations, excluding corticosteroids. Used as nasal decongestants.

C01CA06 - phenylephrine ; Belongs to the class of adrenergic and dopaminergic cardiac


S01FB01 - phenylephrine ; Belongs to the class of sympathomimetics used as mydriatics

and cycloplegics.

S01GA05 - phenylephrine ; Belongs to the class of sympathomimetics used as

ophthalmologic decongestants.

R01AA04 - phenylephrine ; Belongs to the class of topical sympathomimetic agents used as


R01BA03 - phenylephrine ; Belongs to the class of systemic sympathomimetic preparations

used as nasal decongestants.
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VASOPRESSINE

ndication & Dosage Parenteral

Cranialdiabetes insipidus

Adult:As argipressin: 5-20 units SC/IM every 4 hr.

Intravenous

Initial control of variceal bleeding

Adult:As argipressin: 20 units in 100 ml of glucose 5% infused over 15 min.

Contraindications Hypersensitivity. Vascular disease especially coronary artery disease; chronic nephritis (until

reasonable blood-nitrogen conc attained).

Special Precautions Heart failure; migraine; epilepsy; asthma or other conditions which might be exacerbated by

fluid retention; renal impairment; hypertension or other conditions that may worse with BP

increase. Adjust fluid intake to avoid fluid overload. Lactation, pregnancy (especially 3rd

trimester as it may have oxytocic effect).

Adverse Drug

Reactions

Pallor, vomiting, nausea, belching, abdominal cramps, tremour, pounding headache, vertigo,

fluid retention, hyponatraemia, hypersensitivity reaction, sweating, urticaria, gangrene, desire

to defecate, arrhythmias, bradycardia, angina, MI and bronchoconstriction.

Potentially Fatal: Anaphylaxis; cardiac arrest or shock.

Drug Interactions Carbamazepine,chlorpropamide, clofibrate, urea,fludrocortisoneand tricyclic

antidepressants may potentiate the antidiuretic action of vasopressin.Demeclocycline,

noradrenaline, lithium, heparin and alcohol may decrease antidiuretic action of vasopressin.

Ganglionic blockers may increase sensitivity to the pressor effect of vasopressin. Increased

risk of QT prolongation with dolasetron.

Click to view more vasopressin Drug Interactions

Pregnancy Category

(US FDA)

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 1st

trimester (and there is no evidence of a risk in later trimesters).

Storage Intravenous: Store between 15-25C (59-77F). Parenteral: Store between 15-25C (59-

77F).

Mechanism of Action Vasopressin is a posterior pituitary hormone which may be synthetically prepared or

extracted from animals. It exerts direct antidiuretic action on the kidneys by increasing

tubular reabsorption of water. Vasopressin also acts by constricting the peripheral blood

vessels and causes the smooth muscle of the intestine, gall bladder and urinary bladder to

contract. Vasopressin is given parenterally or intranasally in the form of argipressin or

lypressin. Argipressin is a synthetic type of vasopressin derived from most mammals(including man but excluding pig) while lypressin is vasopressin from pig.

MIMS Class Haemostatics/Antidiuretics

ATC Classification H01BA01 - vasopressin ; Belongs to the class of vasopressin and analogues. Used in

posterior pituitary lobe hormone preparations.
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10/62

DOBUTAMINE


Acuteheart failure

Adult: 2.5-10 mcg/kg, up to 0.5-40 mcg/kg according to patient's heart rate, cardiac output,

BP and urine output.

Intravenous

Cardiac stress test

Adult: 5 mcg/kg/min for 8 min using a 1 mg/ml solution, dose is then increased at 5

mcg/kg/min until 20 mcg/kg/min, with each dose being infused for 8 min before the next

increase. Monitor ECG and stop infusion ifarrhythmias, marked ST segmentdepressionor

other adverse effects occur.

Overdosage Symptoms may include anorexia, nausea, vomiting, tremor, anxiety, palpitations, headache,

shortness of breath, and anginal and nonspecific chest pain. Treatment includes

discontinuing drug admin, establishing an airway, ensuring oxygenation and ventilation.

Initiate resuscitative measures immediately. Severe ventricular tachyarrhythmias may be

treated with propranolol or lidocaine. Hypertension usually responds to dose reduction or

therapy discontinuation.

Contraindications Hypersensitivity; idiopathic hypertrophic subaortic stenosis (IHSS).

Special Precautions Correct hypovolaemia prior to treatment. Increased risk of rapid ventricular response in

patients with atrial fibrillation. Insufficient data to determine the safety and efficacy of

dobutamine use after acute MI. Elderly. Neonates. Pregnancy.

Adverse Drug

Reactions

Increased heart rate and BP, ectopic beats, palpitation. Nausea, headache, chest pain,

palpitation, dyspnoea, paraesthesia, leg cramps. Tissue necrosis at site of extravasation.

Potentially Fatal: Cardiac arrhythmias, allergy (rare), MI and hypotension.

Drug Interactions Increased cardiac output when used with nitroprusside. Increased vasopressor effect of

dobutamine when used with bretylium, guanethidine, oxytocic drugs or TCAs.

Click to view more dobutamine Drug Interactions

Pregnancy Category

(US FDA)




in women in the 1st


Storage Intravenous: Store at 15-30C.

Mechanism of Action Dobutamine increases contractility and heart rate by stimulating -adrenergic receptors in the

cardiac tissues.

Absorption: Inactivated in the GI tract (oral).

Metabolism: Converted to 3-O-methyldobutamine.

Excretion: Mainly via urine, via faeces (small amounts); 2 min (elimination half-life).

MIMS Class Cardiac Drugs

ATC Classification C01CA07 - dobutamine ; Belongs to the class of adrenergic and dopaminergic cardiac

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11/62

ATROPINE SULPHATE

Indication & Dosage Parenteral

Premedication in balanced anaesthesia

Adult: 300-600 mcg IM/SC 30-60 minutes beforeanaesthesia. Alternatively, 300-600 mcg IV

immediately before induction ofanaesthesia.

Child: >20 kg: 300-600 mcg; 12-16 kg: 300 mcg; 7-9 kg: 200 mcg; >3 kg: 100 mcg. Doses to

be given via IM/SC admin 30-60 minutes beforeanaesthesia.

Parenteral

Organophosphorus poisoning

Adult: 2 mg IV/IM, every 10-30 minutes until muscarinic effects disappear or atropine toxicity

appears. In severe cases, dose can be given as often as every 5 minutes. In moderate to

severepoisoning, a state of atropinisation is maintained for at least 2 days and continued for

as long as symptoms are present.

Child: 20 mcg/kg given every 5-10 minutes.

Parenteral

Poisoning or overdosage with compounds having muscarinic actions

Adult: 0.6-1 mg IV/IM/SC, repeated every 2 hr.Intravenous

Bradycardia

Adult: 500 mcg every 3-5 minutes. Total: 3 mg.

Max Dosage: 0.04 mg/kg body weight.

Ophthalmic

Inflammatory eye disorders

Adult: Instill 1-2 drops of a 0.5-1% solution up to 4 times daily.

Child:As sulfate: Instill 1-2 drops of a 0.5% soln (or 1 drop of a 1% solution) up to tid.

Ophthalmic

Eye refraction

Adult: Instill 1 drop of a 1% solution bid for 1-2 days before the procedure, or on a singleoccasion 1 hr before the procedure.

Child:As sulfate: Instill 1 or 2 drops of a 0.5% soln (or 1 drop of a 1% solution) bid for 1-3

days before the procedure, with a further dose given 1 hr before the procedure.

Incompatibility: Incompatible with hydroxybenzoate preservatives.

Administration May be taken with or without food. Take w/ food or water.

Overdosage May cause hyperthermia, hypertension, increased respiratory rate, nausea and vomiting.

May also lead to CNS stimulation. Severe intoxication may lead to CNS depression, coma,

respiratory failure and death.

Contraindications Glaucoma, chronic respiratory disease, sick sinus syndrome, thyrotoxicosis, cardiac failure,

pyloric stenosis, prostatic hypertrophy.

Special Precautions Reflux oesophagitis, elderly, infants and children. Pregnancy.

Adverse Drug

Reactions

Dry mouth, dysphagia, constipation, flushing and dryness of skin, tachycardia, palpitations,

arrhythmias, mydriasis, photophobia, cycloplegia, raised intraocular pressure. Toxic doses

cause tachycardia, hyperpyrexia, restlessness, confusion, excitement, hallucinations,

delirium and may progress to circulatory failure and resp depression. Eye drops: Systemic

toxicity esp in children, on prolonged use may lead to irritation, hyperaemia, oedema and
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12/62

conjunctivitis. Increased intraocular pressure. Inhalation: Dryness of mouth, throat.

Potentially Fatal: Atrial arrhythmias, AV dissociation, multiple ventricular ectopics.

Drug Interactions Additive anticholinergic effects withquinidine, antidepressants and some antihistamines.

Click to view more atropine Drug Interactions

Pregnancy Category

(US FDA)





Storage Intravenous: Store at 15-30C. Ophthalmic: Store at 15-30C. Parenteral: Store at 15-

30C.

Mechanism of Action Atropine is an anticholinergic agent which competitively blocks the muscarinic receptors in

peripheral tissues such as the heart, intestines, bronchial muscles, iris and secretory glands.

Some central stimulation may occur. Atropine abolishes bradycardia and reduces heart block

due to vagal activity. Smooth muscles in the bronchi and gut are relaxed while glandularsecretions are reduced. It also has mydriatic and cycloplegic effect.

Absorption: Readily absorbed from the GI tract; also absorbed from mucous membranes,

eye, and through intact skin.

Distribution: Distributes throughout the body and crosses the blood-brain barrier and

placenta.

Metabolism: Incomplete metabolism in the liver.

Excretion: Excreted in urine as unchanged drug and metabolites. Half-life reported to be 4

hr.

MIMS Class Mydriatic Drugs/Antidotes, Detoxifying Agents & Drugs Used in Substance

Dependence/Other Cardiovascular Drugs/Antidotes, Detoxifying Agents & Drugs Used in

Substance Dependence

ATC Classification S01FA01 - atropine ; Belongs to the class of anticholinergics used as mydriatics and

cycloplegics.

A03BA01 - atropine ; Belongs to the class of belladonna alkaloids, tertiary amines. Used in

the treatment of functional gastrointestinal disorders.
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13/62

EPHEDRINE


Diabetic neuropathicoedema

Adult: 30-60 mg tid.

Child:

Intravenous

Reversal of spinal or epidural anaesthesia-inducedhypotension

Adult: 3-6 mg or up to 9 mg in a 3 mg/mL soln given as slow Inj repeated every 3-4 min, as

needed.

Max Dosage: 30 mg.

Administration May be taken with or without food.

Contraindications Hypersensitivity. Hypertension, thyrotoxicosis, BPH. Lactation.

Special Precautions Ischaemic heart disease, hyperthyroidism, diabetes mellitus, hypertension, angle-closure

glaucoma, renal impairment; prostatic enlargement; pregnancy, elderly.

Adverse Drug

Reactions

Anxiety, tachycardia, tremor, dry mouth, hypertension, cardiac arrhythmias, impaired

circulation to the extremities, nervousness, insomnia, palpitations. Difficulty in micturition in

patients with prostatic enlargement. Nasal drops: Local irritation, rebound nasal congestion

and drug-induced rhinitis on prolonged use.

Potentially Fatal: Delusions, hallucinations. Seen with hypersensitivity and overdosage.

Acute CNS and CVS stimulation presenting as vomiting, fever, hypertension, psychosis.

Cardiac arrhythmias.

Drug Interactions Reduces antihypertensive effect of bethanidine andguanethidine. May increase clearance

ofdexamethasone. Increased incidence of adverse effects when used withtheophylline.

Potentially Fatal: Severe HTN when combined with MAOIs or withi 2 wk of discontinuance

of MAOI treatment. Increased risk of arrhythmias with cardiac glycosides,quinidineor

tricyclic antidepressants. Increased vasoconstriction or pressor effects with ergot alkaloids or

oxytocin.

Click to view more ephedrine Drug Interactions

Pregnancy Category

(US FDA)





Storage Intravenous: Store at 15-25C. Oral: Store at 15-25C.

Mechanism of Action Ephedrine has both - and -adrenergic acitivity with pronounced stimulating effects on the

CNS. It increases cardiac output, induces peripheral vasoconstriction, bronchodilation,

reduces intestinal tone and motility, and relaxes the bladder while contracting the sphincter

muscle. It also has stimulant action on the resp center and dilates the pupil witho affecting

light reflexes.

Absorption: Readily and completely absorbed form the GIT (oral).

Metabolism: Hepatic.

Excretion: Via urine (largely as unchanged, small amounts of metabolites); 3-6 hrs

(elimination half-life).
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14/62

MIMS Class Vasoconstrictors

ATC Classification C01CA26 - ephedrine ; Belongs to the class of adrenergic and dopaminergic cardiac


R01AB05 - ephedrine ; Belongs to the class of topical sympathomimetic combination

preparations, excluding corticosteroids. Used as nasal decongestants.

S01FB02 - ephedrine ; Belongs to the class of sympathomimetics used as mydriatics and

cycloplegics.

R03CA02 - ephedrine ; Belongs to the class of adrenergics for systemic use, alpha- and

beta-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.

R01AA03 - ephedrine ; Belongs to the class of topical sympathomimetic agents used as

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15/62

LIDOCAINE


Pulselessventricular fibrillationorventricular tachycardia

Adult:As hydrochloride: 1-1.5 mg/kg repeated as necessary. Max total: 3 mg/kg. For

ventriculararrhythmiasin more stable patients: Usual loading dose: 50-100 mg as an IV inj at

25-50 mg/minute, may repeat once or twice up to a max of 200-300 mg in 1 hr, followed by

1-4 mg/minute via continuous IV infusion. May need to reduce dose if the infusion is longer

than 24 hr.

Hepatic impairment: Reduce dose by 50% in acutehepatitisand decompensated cirrhosis.

Parenteral

Sympathetic nerve block

Adult:As hydrochloride: 50 mg (5 ml) of a 1% solution for cervical block or 50-100 mg (5-10

ml) of a 1% solution for lumbar block.


Epidural

Epidural anaesthesia

Adult:As hydrochloride: 2-3 ml solution administered for each dermatome to beanaesthesized. Recommended doses are: lumbar epidural 250-300 mg (25-30 ml of a 1%

solution) for analgesia and 225-300 mg (15-20 ml of a 1.5% solution) or 200-300 mg (10-15

ml of a 2% solution) foranaesthesia; for thoracic epidural: 200-300 mg of a 1% solution. For

obstetric caudal analgesia, up to 300 mg (30 ml of a 0.5% or 1% solution); for surgical caudal

analgesia: 225-300 mg (15-20 ml of a 1.5% solution). For continuousepidural anaesthesia,

not to repeat max doses more frequently than 1.5 hrly.


Intraspinal

Spinal anaesthesia

Adult:As hyperbaric solution of 1.5% or 5% lidocaine in 7.5% glucose solution. Normal

vaginal delivery: 50 mg (1 ml) of a 5% solution or 9-15 mg (0.6-1 ml) of a 1.5% solution.Caesarian operation: Up to 75 mg (1.5 ml) of a 5% solution. Other surgical procedures: 75-

100 mg (1.5-2 ml).


Intravenous

Intravenous regional anaesthesia

Adult: 50-300 mg (10-60 ml) of a 0.5% solution withoutadrenaline; max dose: 4 mg/kg.


Urethral

Surface anaesthesia

Adult:As 2% gel: Female: 60-100 mg inserted into the urethra several minutes before

examination. Male: 100-200 mg before catheterisation and 600 mg before sounding or

cystoscopy.


Intramuscular

Emergency treatment of ventricular arrhythmias

Adult:As hydrochloride: 300 mg injected into the deltoid muscle, repeat after 60-90 minutes

if necessary.


Parenteral
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Percutaneousinfiltration anaesthesia

Adult:As hydrochloride: 5-300 mg (1-60 ml of a 0.5% solution or 0.5-30 ml of a 1% solution).


Parenteral

Peripheral nerve block

Adult:As hydrochloride: For brachial plexus block: 225-300 mg (15-20 ml) of a 1.5%solution; for intercostal nerve block: 30 mg (3 ml) of a 1% solution; for paracervical block: 100

mg (10 ml) of a 1% solution on each side, repeated not more frequently than every 90

minutes; for paravertebral block: 30-50 mg (3-5 ml) of a 1% solution; for pudendal block: 100

mg (10 ml) as a 1% solution on each side; for retrobulbar block: 120-200 mg (3-5 ml) of a 4%

solution.


Injection

Pupil dilatation during phacoemulsificationcataractsurgery

Adult:As a 1% ophthalmic preservative-free solution (often used in combination with

phenylephrine and cyclopentolate). To be injected into the anterior chamber of the eye at the

beginning of the procedure.

Mouth/Throat

Surface anaesthesia

Adult: For pain: 300 mg (15 ml) of 2% solution rinsed and ejected for mouth andthroat pain;

or gargled and swallowed if necessary for pharyngeal pain. Not to be used more frequently

than every 3 hr. Max (topical oral solution): 2.4 g/day. Before bronchoscopy, bronchography,

laryngoscopy, oesophagoscopy, endotracheal intubation, and biopsy in the mouth and throat:

40-300 mg (1-7.5 ml) of 4% solution. For dentistry and otorhinolaryngology procedures: 10-

50 mg of 10% solution sprayed to mucous membrane. For laryngotracheal anaesthesia: 160

mg of 4% solution sprayed or instilled as a single dose into the lumen of the larynx and

trachea.


OphthalmicSurface anaesthesia

Adult:As hydrochloride 4 % with fluorescein: 1 or more drops as required.

Child:As hydrochloride 4 % with fluorescein : As directed by physician.

Topical/Cutaneous

Surface anaesthesia

Adult:As eutectic mixture containing lidocaine base 2.5% and prilocaine base 2.5%: Apply

cream to skin under an occlusive dressing before procedure. Use without an occlusive

dressing forgenital warts.


Rectal

Haemorrhoids

Adult:Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day.

Child: 12 yr: Apply topically to clean, dry area or using applicator, insert rectally, up to 6

times/day.


Rectal

Perianalpainand itching

Adult:Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day.
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17/62

Child: 12 yr: Apply topically to clean, dry area or using applicator, insert rectally, up to 6

times/day.


Reconstitution: Standard diluent: 2 g/250 ml dextrose 5%.

Incompatibility: Y-site incompatibility: Amphotericin B cholesteryl sulfate complex,thiopental. Syringe incompatibility: Cefazolin. Admixture incompatibility: Phenytoin,

amphotericin B, dacarbazine, methohexital.

Overdosage Severe hypotension, asystole, bradycardia, apnoea, seizures, coma, cardiac arrest,

respiratory arrest, and death.

Contraindications Hypovolaemia; heart block or other conduction disturbances.

Special Precautions Hepatic or renal impairment; CHF and following cardiac surgery; bradycardia; respiratory

depression; porphyria; elderly or debilitated patients; pregnancy.

Adverse Drug

Reactions

Dizziness, paraesthesia, drowsiness, confusion, respiratory depression and convulsions.

Potentially Fatal: Hypotension and bradycardia leading to cardiac arrest; anaphylaxis.

Drug Interactions Additive cardiac effects with IV phenytoin. Effects antagonized by hypokalaemia caused by

acetazolamide, loop diuretics and thiazides. Dose requirements may be increased with long-

term use ofphenytoinand other enzyme-inducers.

Potentially Fatal:Cimetidineandpropranololincrease plasma concentration and toxicity.

Increased risk of myocardial depression with beta blockers and other antiarrhythmics.

Click to view more lidocaine Drug Interactions

Food Interaction Decreased levels with St John's wort.

Lab Interference IM admin of lidocaine increases creatine phosphokinase levels interfering with diagnosis of

MI.

Pregnancy Category

(US FDA)

ROUTE(S) : Intradermal / Topical/Cutaneous




in women in the 1st


ROUTE(S) : Parenteral

As LA & cardiac drug.


are no controlled studies in pregnant women or animal-reproduction studies have shown anadverse effect (other than a decrease in fertility) that was not confirmed in controlled studies

in women in the 1st


Storage Epidural: Stable at room temperature. Intramuscular: Stable at room

temperature. Intraspinal: Stable at room temperature. Intravenous: Stable at room

temperature. Mouth/Throat: Stable at room temperature. Ophthalmic:Store at 15-25C.

Protect from light. Discard after use. Parenteral: Stable at room temperature. Rectal: Stable

at room temperature. Topical/Cutaneous: Stable at room temperature. Urethral: Stable at
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18/62

room temperature.

Mechanism of Action Lidocaine is an amide type local anaesthetic. It stabilises the neuronal membrane and

inhibits sodium ion movements, which are necessary for conduction of impulses. In the heart,

lidocaine reduces phase 4 depolarisation and automaticity. Duration of action potential and

effective refractory period are also reduced.

Onset: 45-90 sec.

Duration: 10-20 min.

Absorption: Readily absorbed from the GI tract, mucous membranes, damaged skin, inj

sites, including muscle; poor through intact skin.

Distribution: Crosses the placenta, blood-brain barrier and enters breast milk. Protein-

binding: 66% (1-acid glycoprotein).

Metabolism: 90% hepatic; converted to monoethylglycinexylidide and glycinexylidide. First-

pass metabolism is extensive, bioavailability after oral dose is approx 35%.

Excretion: Via urine (


19/62

DEXAMETHASONE


Anti-inflammatory

Adult: 0.75-9 mg daily in 2-4 divided doses; may also be given via IM/IV admin.

Child: 1 mth-18 yr: 10-100 mcg/kg daily in 1-2 divided doses via oral admin, adjusted

according to response; up to 300 micrograms/kg daily may be used in emergency situations.

Oral

As a screening test for Cushing's syndrome

Adult: 0.5 mg every 6 hr for 48 hr after determining baseline 24-hr urinary 17-

hydroxycorticosteroid (17-OHCS) concentrations. During the second 24 hr of

dexamethasone admin, urine is collected and analysed for 17-OHCS. Alternatively, after a

baseline plasma cortisol determination, 1 mg may be given at 11 pm and plasma cortisol

determined at 8 am the next morning. Plasma cortisol and urinary output of 17-OHCS are

depressed after dexamethasone admin in normal individuals but remain at basal levels in

patients with Cushing's syndrome.

Oral

Acute exacerbations inmultiple sclerosisAdult: 30 mg daily for 1 wk followed by 4-12 mg daily for 1 mth.

Child: 1 mth-12 yr: 100-400 mcg/kg daily in 1-2 divided doses; 12-18 yr: Initially 0.5-24 mg

daily. Max. 24 mg daily.

Parenteral

Cerebral oedemacaused by malignancy

Adult:As phosphate: 10 mg IV followed by 4 mg IM every 6 hr until response is achieved,

usually after 12-24 hr. May reduce dosage after 2-4 days then gradually discontinued over 5-

7 days. In severe cases, an initial dose of 50 mg IV may be given on day 1, with 8 mg every

2 hr, reduced gradually over 7-13 days. Maintenance dose: 2 mg 2-3 times daily.

Child:As phosphate: 35 kg:Initially 25 mg, then 4 mg every 2 hr for 3 days, then 4 mg every 4 hr for 1 day, then 4 mg

every 6 hr for 4 days, then decrease by 2 mg daily. Doses are given via IV inj.

Intra-articular

Inflammatory joint diseases

Adult: 0.8-4 mg depending on the size of the affected joint. For soft-tissue inj, 2-6 mg may

be used. May repeat inj every 3-5 days to every 2-3 wk.

Intravenous

Unresponsiveshock

Adult:As phosphate: Initially, 40 mg or 1-6 mg/kg as a single IV inj, may repeat every 2-6 hr.

Continue high-dose treatment only until patient's condition has stabilised and not to be

continued beyond 48-72 hr.

Intravenous

Bacterial meningitis

Adult: 0.15 mg/kg 4 times daily, to be given 10-20 min before or with the 1st dose of anti-

infective treatment. Treatment should be given for the first 2-4 days of the anti-infective

treatment.

Child:As phosphate: 2 mth-18 yr: 150 mcg/kg every 6 hr for 4 days, starting before or with

1st dose of antibacterial treatment.

Intravenous
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Prophylaxis ofnausea and vomitingassociated with cytotoxic therapy

Adult: Prevention: 10-20 mg 15-30 minutes before admin of chemotherapy on each

treatment day. For continuous infusion regimen: 10 mg every 12 hr on each treatment day.

For midly emetogenic regimen: 4 mg every 4-6 hr.

Ophthalmic

Ocular inflammationAdult:As 0.1% suspension: Apply 1-2 drops into the affected eye/s 4-6 times daily in mild

disease, up to hrly admin in more severe disease. As 0.05% ointment: Apply 0.5-1 inch

ribbon of ointment into the conjunctival sac(s) up to 4 times daily. Reduce to once daily

dosing once conditon has improved.

Administration Should be taken with food.

Overdosage Treatment is supportive and symptomatic. In acute overdosage, gastric lavage or emesis

may be used.

Contraindications Hypersensitivity; active untreated infections; ophthalmic use in viral, fungal disease of the

eye.

Special Precautions Patients with hypothyroidism; cirrhosis, hypertension, CHF, ulcerative colitis, thromboembolicdisorders, osteoporosis, glaucoma, cataracts or TB of the eye, diabetes, peptic ulcer. Monitor

blood glucose levels in diabetics and coagulation indices in patients on warfarin. Elderly,

children and adolescent; pregnancy and lactation.

Adverse Drug

Reactions

Growth retardation, osteoporosis, peptic ulcer, glaucoma and subcapsular cataracts,

vertebral compression fractures. Cushing-like features, pancreatic dysfunction and

pancreatitis, GI upsets, increased appetite, increased fragility of the skin. Increased

susceptibility to infection. Topical application: Dermal atrophy, local irritation, folliculitis,

delayed wound healing, systemic absorption and toxicity with occlusive dressing on

application to large areas of the body and broken skin. Topical application to eye: Corneal

ulcers, glaucoma and reduced visual ability. Inhalation: Hoarseness, candidiasis of mouth

and throat. Intra-articular inj: Aseptic necrosis of bone and joint damage.Potentially Fatal: HPA supression; CV collapse on rapid IV admin.

Drug Interactions Increased risk of hypokalaemia when used concurrently with potassium-depleting drugs such

asamphotericinB and loop diuretics. Reduces efficacy of isoniazid, salicylates, vaccines and

toxoids. Increased activity of dexamethasone andcyclosporinwhen used together.

Concurrent use withaspirinor ethanol may lead to increased GI side effects.

Potentially Fatal: Reduced efficacy in combination withephedrine,

cholestyramine,phenytoin,phenobarbitalandrifampicin.

Click to view more dexamethasone Drug Interactions

Food Interaction Dexamethasone interferes with calcium absorption. Limit caffeine.

Pregnancy Category(US FDA)

ROUTE(S) : Ophthalmic





ROUTE(S) : Oral / Parenteral
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D in 1st trimester.



in women and animals are not available. Drugs should be given only if the potential benefitjustifies the potential risk to the foetus.

Storage Intra-articular: Store at 15-30C. Intravenous: Store at 15-30C. Ophthalmic: Store at 15-

30C. Oral: Store at 15-30C. Parenteral: Store at 15-30C.

Mechanism of Action Dexamethasone is a synthetic glucocorticoid which decreases inflammation by inhibiting the

migration of leukocytes and reversal of increased capillary permeability. It suppresses normal

immune response.

Onset:As acetate: Prompt.

Duration: 72 hr.

Absorption: Readily absorbed from the GI tract (Oral).

Distribution: Readily crosses the placenta. Protein binding: About 77%.

Metabolism: Hepatic.

Excretion: Via urine (65% of the dose within 24 hr). Half-life: About 190 min.

MIMS Class Corticosteroid Hormones/Eye Corticosteroids/Topical Corticosteroids

ATC Classification D10AA03 - dexamethasone ; Belongs to the class of topical corticosteroids used in the

treatment of acne.

S02BA06 - dexamethasone ; Belongs to the class of corticosteroids used in the treatment of

inflammation of the ear.

D07XB05 - dexamethasone ; Belongs to the class of moderately potent (group II)

corticosteroids in other combinations. Used in the treatment of dermatological diseases.

A01AC02 - dexamethasone ; Belongs to the class of local corticosteroid preparations. Used

in the treatment of diseases of the mouth.

S03BA01 - dexamethasone ; Belongs to the class of corticosteroids used in ophthalmologic

and otologic preparations.

R01AD03 - dexamethasone ; Belongs to the class of topical corticosteroids used for

prophylaxis and treatment of allergic rhinitis.

S01CB01 - dexamethasone ; Belongs to the class of corticosteroids/antiinfectives/mydriatics

combinations. Used in the treatment of eye diseases.

D07AB19 - dexamethasone ; Belongs to the class of moderately potent (group II)

corticosteroids. Used in the treatment of dermatological diseases.

S01BA01 - dexamethasone ; Belongs to the class of corticosteroids. Used in the treatment of

inflammation of the eye.

H02AB02 - dexamethasone ; Belongs to the class of glucocorticoids. Used in systemic

corticosteroid preparations.

C05AA09 - dexamethasone ; Belongs to the class of products containing corticosteroids for

topical use. Used in the treatment of hemorrhoids and anal fissures.
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RANITIDINE


Benign gastric and duodenal ulceration

Adult: Initially, 300 mg as a single daily dose at bedtime or 150 mg bid; 300 mg bid for 4 wk

may be used induodenal ulcerto improve healing). Treatment duration: 4-8 wk for benign

gastric and duodenal ulceration; up to 8 wk in NSAID-associated ulceration. For prevention

of NSAID-associated ulceration: 150 mg bid.

Child: 3-12 yr: 2-4 mg/kg (max: 150 mg) bid for 4-8 wk.

Renal impairment: Dosage reduction is required in severerenal impairment.

CrCl (ml/min) Dosage Recommendation

20 Dosage should be halved.

Oral

H.pylori infection

Adult: 300 mg once daily or 150 mg bid in combination with amoxicillin 750 mg tid and

metronidazole 500 mg tid given for 2 wk. Treatment with ranitidine may be continued for a

further 2 wk.




Oral

Gastro-oesophageal refluxdisease

Adult: 150 mg bid or 300 mg at bedtime for up to 8 wk, may increase to 150 mg four times

daily for 12 wk in severe cases.

Child: 5-10 mg/kg daily, given in 2 divided doses.




Oral

Hypersecretory conditions

Adult: Initially, 150 mg bid/tid increased to 6 g daily if necessary.




OralAcid aspiration duringgeneral anaesthesia

Adult: 150 mg given 2 hr before induction ofanaesthesiaand preferably, an additional dose

on the previous evening.



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