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Medical Pharmacology Ovidius 2014

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Adrenalin – epinephrine
Naphazoline
Phenylephrine
Ephedrine
Clonidine
Isoprenaline
Salbutamol
Prazosin
Propranolol

10. Atenolol
11. Labetalol
12. Timolol
13. Atropine
14. Pilocarpine
15. Neostigmine
16. Pirenzepine
17. Ipratropium Bromide

1.
Epinephrine is one of four catecholamines (epinephrine, norepinephrine, dopamine,
and dobutamine) commonly used in therapy. The first three catecholamines occur
naturally in the body as neurotransmitters; the latter is a synthetic compound.
Epinephrine is synthesized from tyrosine in the adrenal medulla and released, along
with small quantities of norepinephrine, into the bloodstream.
a) Pharmacological class : Direct acting Sympathomimetic or Direct acting Adrenergic
Agonist
b) Mechanism of Action : Epinephrine interacts with both α and β receptors. At low
doses, β effects (vasodilation) on the vascular system predominate, whereas at high
doses, α effects (vasoconstriction) are strongest.

c) Pharmacologic effects :

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II.

III.

IV.

Cardiovascular:
o The major action.
o Strengthens the contractility of the myocardium (positive inotropic action)
o Increases its rate of contraction (positive chronotropic action).
o Cardiac output increases.
o Epinephrine constricts arterioles in the skin, mucous membranes, and viscera and it
dilates vessels going to the liver and skeletal muscle.
o Renal blood flow is decreased.
o Increase in systolic blood pressure, coupled with a slight decrease in diastolic
pressure.
Respiratory:
o powerful bronchodilation by acting directly on bronchial smooth muscle. This action
relieves all known allergic- or histamine-induced bronchoconstriction. In the case of
anaphylactic shock, this can be lifesaving.
o In acute asthmatic attack, epinephrine rapidly relieves the dyspnea.
Hyperglycemia
o significant hyperglycemic effect because of increased glycogenolysis in the liver,
increased release of glucagon and a decreased release of insulin
Lipolysis:
o Epinephrine initiates lipolysis through its agonist activity on the receptors of adipose
tissue

000) can also be used topically to vasoconstrict mucous membranes to control oozing of capillary blood. The effect of the drug is to greatly increase the duration of the local anesthesia. subcutaneous 1/3 vial every 84h . V. It does this by producing vasoconstriction at the site of injection. thereby allowing the local anesthetic to persist at the injection site before being absorbed into the circulation and metabolized. Within a few minutes after subcutaneous administration. Nasal solution.000 parts epinephrine.s. e) Contraindications : Hypersensitivity Hypovolemic shock Coronary insufficiency Hypertension f) Adverse Effects :  Anxiety  Headache  Cerebral hemorrhage  Cardiac arrhythmias  Pulmonary edema from pulmonary hypertension g) Pharmacography : 1 mg/mL IM or subcutaneous. Glaucoma: In ophthalmology. III.d) Therapeutic uses (indications) : I. It reduces the production of aqueous humor by vasoconstriction of the ciliary body blood vessels. Oral inhalation h) Prescription: Dg/ Asthma attacks Rp/epinephrine vials 1mg/ml Nr. Very weak solutions of epinephrine (1:100. I D. IV. Cardiac arrest: Epinephrine may be used to restore cardiac rhythm in patients with cardiac arrest regardless of the cause. 2% epinephrine solution may be used topically to reduce intraocular pressure in open-angle glaucoma. Anaphylactic shock: Epinephrine is the drug of choice for the treatment of Type I hypersensitivity reactions in response to allergens. Administration may be repeated after a few hours. Anesthetics: Local anesthetic solutions usually contain 1:100. greatly improve respiratory exchange is observed. Bronchospasm: Epinephrine is the primary drug used in the emergency treatment of any condition of the respiratory tract when bronchoconstriction has resulted in diminished respiratory exchange. II.

sweating.s. The sympathomimetic action constricts the smaller arterioles of the nasal passages.1% . hyperglycemia g) Pharmacography : Ophthalmic drops 0. This activates the adrenal system to yield systemic vasoconstrction. It also decreases itching and irritation of the eyes. cardiac irregularities. the result is a decrease in blood flow in the nasal passages and consequently decreased nasal congestion.1% Nr. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out. d) Therapeutic uses (indications) : Naphazoline is primarily indicated in conditions like Corneal vascularity. thus less discharge is made. Hyperaemia. weakeness. increased intraocular pressure Systemic : Dizziness. Ophthalmic use causes constriction of blood vessels in the eyes. I D. producing a decongesting effect. thereby decreasing nasal congestion and inducing constriction around the conjunctiva. Headache. It is presumed that this effect is due to direct stimulation action of the drug upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in decreased conjunctival congestion. In producing vasoconstriction. Mydriasis. keratitis. nausea . Constricts the vascular system of the conjunctiva. Nasal drops h) Prescription Dg/Rhinitis Rp/Naphazoline sol 0.a) Pharmacological class : It is a sympathomimetic agent with marked alpha adrenergic activity b) Mechanism of Action : Naphazoline is a direct acting sympathomimetic drug. and can also be given in adjunctive therapy as an alternative drug of choice in Sinusitis e) Contraindications : In narrow angle glaucoma or in persons with hypersensitivity f) Adverse Effects : Ocular : severe hypertensive crisis. irritation. lacrimation. nervousness. redness. which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. c) Pharmacologic effects : induce systemic vasoconstriction. Itching. Nasal congestion. Externally 1 drop intranasal 3times/day .

cream h) Prescription Dg/ Hypotension Rp/Phenylephrine vial 10mg/ml Nr. Phenylephrine produces its local and systemic actions by acting on α1-adrenergic receptors peripheral vascular smooth muscle. IM or subcutaneous: 2 to 5 mg every 1 to 2 hours as needed.s. this leads to decreased edema and increased drainage of the sinus cavities.2-0. α1-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. iii. prolongation of spinal anaesthesia. Phenylephrine decreases nasal congestion by acting on α1-adrenergic receptors in the arterioles of the nasal mucosa to produce constriction. Also causes pulmonary vessel constriction and subsequent increase in pulmonary arterial pressure. and to increase blood pressure as an aid in the diagnosis of heart murmurs. Tablets 10mg-20mg v. IV ½ vial rapidly .25mg/ 0. Syrup 1.5 mg/dose vi. Drops. paroxysmal supraventricular tachycardia. d) Therapeutic uses (indications) : It is often used topically on the nasal mucous membranes and in ophthalmic solutions for mydriasis. hypotension during spinal anaesthesia. symptomatic relief of external or internal hemorrhoids. Stimulation of the α1-adrenergic receptors results in contraction arteriolar smooth muscle in the periphery. synthetic adrenergic agonist b) Mechanism of Action : Binds primarily α1 receptors. Decreases edema and increased drainage of sinus cavities.. I D. opth. but may also be useful in treating hypotension and shock. e) Contraindications : Hypertention f) Adverse Effects :Large doses cause hypertensive headache and cardiac irregularities. g) Pharmacography : i. vii.8ml ii. It has no effect on the heart itself but rather induces reflex bradycardia when given parenterally. c) Pharmacologic effects : Phenylephrine is a vasoconstrictor that raises both systolic and diastolic blood pressures.a) Pharmacological class : is a direct-acting. iv.. Vasoconstriction in the mucosa of the respiratory tract leads to decreased edema and increased drainage of sinus cavities. It is mainly used to treat nasal congestion. supository. IV: 0. oint.

The ephedrine. phaeochromocytoma asymmetric septal hypertrophy. prostatic hypertrophy. but the bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline or noradrenaline from ephedrine. appetite suppressant. Ephedrine's action as an agonist at most major noradrenaline receptors and its ability to increase the release of both dopamine and to a lesser extent. hypersensitivity to ephedrine or other stimulants. mixed with noradrenaline. concentration aid. hyperthyroidism. closed angle glaucoma. Increase peripheral resistance and cause cardiac stimulation e. c. .it produces direct stimulation of adrenergic R. b) Mechanism of Action : direct and indirect actions on the adrenergic receptor system. acidosis. diabetes mellitus. e) Contraindications : Ephedrine should not be used in conjunction with certain antidepressants. hypoxia. Bronchodialation f. is transported through the noradrenaline reuptake complex and packaged (along with real noradrenaline) into vesicles that reside at the terminal button of a nerve cell. agitation. during delivery if maternal BP > 130/80 mmHg. Second. Its primary action is indirect. d. a) Pharmacological class : Mixed action Adrenergic agonist OR mixed-acting symphatomimetic agent( with both. impaired adrenal. Ephedrine should be used with caution in patients with inadequate fluid replacement . nausea. In IV administration it has the same effects with epinephrine . d) Therapeutic uses (indications) : Ephedrine commonly used as a stimulant. direct and indirect actions). c) Pharmacologic effects : a. decongestant. and lactation. Ephedrine increases post-synaptic noradrenergic receptor activity by (weakly) directly activating post-synaptic α-receptors and β-receptors.4.it causes the release of NE from storage in nerve terminals. cardiovascular disease. which is part of the sympathetic nervous system.hypertension. It’s potency is 1/250 that of epinephrine in producing an equivalent pressor response. Its causes CNS stimulation: insomnia. function. b. serotonin by the same mechanism is presumed to have a major role in its mechanism of action. and to treat hypotension associated with anaesthesia. nervousness. hypercapnia. g. the pressor response occurs more slowly and lasts 10 times longer. Tachyphylaxis with repeated administration. apparently by competing with NE for transport into granules. tachyarrhythmias or ventricular fibrillation.

I D. dry mouth g) Pharmacography : Oral :Tablet. insomnia. pulmonary edema o Miscellaneous: dizziness. powder Injectable : IV and IM h) Prescription Dg/Rhinitis Rp/Ephedrine sol. difficulty urinating is not uncommon. mania/hallucinations (rare except in previously existing psychiatric conditions).delusions. cardiac arrhythmias. Also. formication (may be possible. headache. intranasally 2 drops per nosetrill 2 times / day for 1 week . mimicking the effects of sympathetic nervous system stimulation. acne vulgaris o Gastrointestinal: nausea o Genitourinary: decreased urination due to vasoconstriction of renal arteries. capsule 25mg.s. hostility. vasoconstriction with hypertension o Dermatological: flushing. panic. angina pectoris.f) Adverse Effects : o Cardiovascular: tachycardia. confusion. as alpha-agonists such as ephedrine constrict the internal urethral sphincter. tremor. 1% Nr. sweating. o Nervous system: restlessness. hyperglycemic reactions. agitation o Respiratory: dyspnea. mild euphoria. but lacks documented evidence) paranoia.

Skin reactions (if given transdermally).4mg h) Prescription Dg/ ADHD Rp/Clonidine. anxiety/panic disorder. avoid abrupt withdrawal. Its mechanism of action in the treatment of ADHD is to increase noradrenergic tone in the prefrontal cortex (PFC) directly by binding to postsynaptic α2 adrenergic receptors and indirectly by increasing norepinephrine input from the locus coeruleus. Nausea/vomiting. Raynaud's phenomenon. alcohol and nicotine (smoking). Headache (dosedependent).s.2mg. Sedation (dose-dependent). It can alleviate opioid withdrawal symptoms by reducing the sympathetic nervous system response such as tachycardia and hypertension. 1 per day . lowering blood pressure d) Therapeutic uses (indications) : Used to treat high blood pressure. thus inhibiting the release of norepinephrine (NE)  Decreases peripheral vascular resistance. Hallucination. Paraesthesia. as well as reducing sweating. XXX D. Sinus bradycardia. Also can be used for severe Dysmenorrhea e) Contraindications : hypersens.Orthostatic hypotension . and general restlessness. Urticaria (hives) g) Pharmacography : Epidural inj. This binding decreases presynaptic calcium levels.5. patch 0.2mg-0. Constipation. Clonidine may be used to ease withdrawal symptoms associated with the long-term use of narcotics. c) Pharmacologic effects :  Decreases presynaptic calcium levels. anticoagulant use (epidural use). and certain pain conditions. a) Pharmacological class : α2 Direct Acting Adrenergic Agonist b) Mechanism of Action : Clonidine treats high blood pressure by stimulating α2-receptors in the brain. patch 0.coagulation disorder (epidural use). Hypotension Common : Anxiety. Dry mouth. caution in elderly pts caution if cardiovascular dz or severe CAD or if recent MI or cardiac conduction disturbance or if renal impairment or if depression or if cerebrovascular dz or caution if CNS depressant use or alcohol use f) Adverse Effects : Very common : Dizziness . Nightmare. It has specificity towards the presynaptic α2-receptors in the vasomotor center in the brainstem.2mg Nr. Attention deficit hyperactivity disorder. tablet 0. lowering blood pressure.. which decreases peripheral vascular resistance. Malaise Weight gain/loss Uncommon: Delusional perception. thus inhibiting the release of norepinephrine (NE). to drug/class/component. Dermal placement. The net effect is a decrease in sympathetic tone. Fatigue. Pruritus (itchiness). hot and cold flashes.

sol. It can be employed to stimulate the heart in emergency situations. Isoproterenol also dilates the arterioles of skeletal muscle (β2 effect). is useful in the treatment of atrioventricular block or cardiac arrest.and b2-adrenergic receptors. resulting in decreased peripheral resistance. It is as active as epinephrine in this action and. c) Pharmacologic effects : o Cardiovascular: Isoproterenol produces intense stimulation of the heart to increase its rate and force of contraction. e) Contraindications : Isoprenaline should not be administered to patients with myocardial ischemia. This action lasts about 1 hour and may be repeated by subsequent doses. Its nonselectivity is one of its drawbacks and the reason why it is rarely used therapeutically. Other effects: Other actions on β receptors. inhalatory 1 puff every 8h / 7days . such as increased blood sugar and increased lipolysis. therefore. it may increase systolic blood pressure slightly. gel h) Prescription Dg/Athma Rp/Isoprenaline . a) Pharmacological class : It is a non-selective beta-adrenergic agonist b) Mechanism of Action : Isoproterenol is a direct-acting synthetic catecholamine that predominantly stimulates both b1. but it greatly reduces mean arterial and diastolic blood pressure.6. spray. o o Pulmonary: A profound and rapid bronchodilation is produced by the drug. causing increased cardiac output. Cardiac arrest was noted in several instances f) Adverse Effects :      Anxiety Headache Cerebral hemorrhage Cardiac arrhythmias Pulmonary edema from pulmonary hypertension g) Pharmacography : IM . Because of its cardiac stimulatory action. Isoproterenol is as active as epinephrine and rapidly alleviates an acute attack of asthma when taken by inhalation (which is the recommended route). d) Therapeutic uses (indications) : Isoproterenol is now rarely used as a broncho-dilator in asthma. MDI 80µg Nr. Its action on alpha receptors is insignificant.s. I D. can be demonstrated but are not clinically significant.

caution in patients with CV disease or hyperthyroidism.s. regular use of short-acting beta 2 agonists can be associated with increased bronchial hyperresponsiveness to methacoline challenge ii.Oral: Liquid sol and tab. tolerance iii. inhibits microvascular leakage. IM and IV sol. Binding of the drug to β2 receptors in the lungs results in relaxation of bronchial smooth muscles.7. a) Pharmacological class : short-acting. are not recommended for acute asthma e) Adverse Effects : i. Tremor. and enhances mucociliary clearance.cardiac R c) Therapeutic uses (indications) : bronchial asthma. A lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation. COPD d) Contraindications : sensitivity to drug. due to stimulation of skeletal muscle f) Pharmacography : Respiratory as aerosols inhalants. but also are available as oral powder and solution. because they can have minimal effects on β1 R of the heart. salbutamol inhibits the release of bronchoconstricting agents from mast cells. selective β2-adrenergic receptor agonist b) Mechanism of Action : it stimulates β2-adrenergic receptors. g) Prescription : Dg/Asthma Rp/Salbutamol MDI 90µg Nr. c) Pharmacologic effects : Being β2 agonists they have a relaxing effect on bronchial smooth muscle and show little effect on cardiac β1. It Inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. I D. 1 puff when needed no more than 8puffs per day . bronchospasm. In addition to bronchodilation. iv. inhalatory.

a) Pharmacological class : selective α1. g) Pharmacography : Oral – caps and tablets 5mg h) Prescription Dg/Hypertension Rp/Prazosin tab. so that it causes only a small degree of tachycardia It decreases arterial pressure with little change in cardiac output. and the first minimal dose to be administered in the evening. to avoid this effect doses are increased slowly. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine). resulting in peripheral vasodilation. till the therapeutic dose.XXX D.s.adrenergic antagonist b) Mechanism of Action : Acts by inhibiting the postsynaptic α1-adrenoceptors on vascular smooth muscle. neurotransmitter feed-back inhibition is maintained. 5mg Nr. orally 1cap/day for 30 days . heart rate and right atrial pressure d) Therapeutic uses (indications) :    Mild-moderate hypertension Congestive heart failure Symptomatic benign prostatic hyperplasia e) Contraindications :  Hypersensitivity to drug/class/component  caution in elderly pts  caution if cataract surgery f) Adverse Effects :  First dose effect = postural hypotension. c) Pharmacologic effects :    Reduces vascular tone in both resistance and capacitance vessels Because it has no effect on α2-R.

f) Adverse effects: .Rapid withdrawl can lead to “supersensitivity”= up-regulation. b) Mechanism of action: non-selective β blocker. o Bradycardia (<60 beats/minute) o Sick sinus syndrome o Atrioventricular block (second or third degree) o Shock and Severe hypotension h) RP/ Dg/Hypertension Rp/Propranolol tab.s.Management of hypertrophic cardiomyopathies to reduce the force of myocardial contractions .It interfere with carbohydrate and fat metabolism e) pharmacography and modality of administration:  Oral: Tablet 40mg .Prolong use: fatigue.Prophylaxis of migraine headaches d) Pharmacologic effects : . fever. arrhythmias or myocardial infarction . purpura . of β-adrenergic R.Cautions in asthmatics and in diabetic patients treated with insulin. capsule 40mg  Intravenous: solution. vascular and uterine) receptor sites.Hypertension.Prophylaxis of supra and ventricular arrhythmias . peripheral arterial insufficiency .It can induce heart failure . . because it alters renal hemodynamics .a) Pharmacological class: Sympathetic antagonist. Propanolol blocks stimulation of β1adrenergic (myocardial) and beta2-adrenergic (pulmonary.It increases airway resistance by β2 blockade . slows heart rate and reduces blood pressure. which can provoke anginal attacks. depression.Management of hyperthyroidism and anxiety states to decrease the heart rate .Prophylaxis of angina pectoris . except to the brain .C-I in patients with Raynaud syndrome g) Contraindications: o Reversible airways disease. This action decreases cardiac output. 40mg Nr.Rash.It inhibits the renal secretion of renin.Long-term prophylaxis in patients who have had myocardial infarction and are at high risk for infarction or sudden death . orally 1tab/12h for 30 days . nightmares. sexual disfunctions.It depresses Na+ excretion.It reduces blood flow to most tissues.It decreases the heart rate and cardiac output and prolongs systole. . particularly asthma or COPD. c) Therapeutic use: .It decreases total coronary blood flow and oxygen consumption . or persons with hypoglycemia . often combined with a diuretic . LX D.

I. inhibiting sympathetic stimulation--> reduction in resting heart rate.s. cardiac output. diabetes mellitus. nightmares o Edema g) Contraindications: atenolol should not be provided to patients with:  avoid abrupt withdrawal  caution if peripheral vascular disease. orally 1tab/day for 30 days .a) Pharmacological class: Sympathetic antagonist b) Mechanism of action: Selective β1 receptor antagonist. renal impairment. systolic and diastolic blood pressure. o It decreases total coronary blood flow and oxygen consumption o It inhibits the renal secretion of renin. d) Pharmacologic effects: o It decreases the heart rate and cardiac output and prolongs systole. o It depresses Na+ excretion. lack of energy o impotence o rhinitis o depression o confusion o insomnia. because it alters renal hemodynamics e) Pharmacography and modality of administration: Tablets 50mg-25mg . o Type II diabetes.V Injection f) Adverse effects: Unlike propranolol. Developed as a remplacement for propranolol in the treatment of hypertension. constipation. Atenolol competes with sympathomimetic neurotransmitters for binding at β1adrenergic receptors in the heart and vascular smooth muscle. pregnancy and breastfeeding 8. o Long-term prophylaxis in patients who have had myocardial infarction and are at high risk for infarction or sudden death o Prophilaxis of supraventricular and ventricular tachycardia. and reflex orthostatic hypotension. fatigue. o Grave's disease until antithyroid medication can take effect. bronchospastic disease. dry mouth o dizziness or faintness. c) Therapeutic use: o Hypertension. weakness. atenolol does not pass through the blood–brain barrier thus avoiding various central nervous system side effects. XXX D. o Prophilaxis of angina pectoris. RP/ Dg/Hypertension Rp/Atenolol tab 50mg Nr. o indigestion. thyroid disorder.

hypotension or cardiogenic shock. g.a. o Avaiable as i.v. c. slows heart rate and reduces blood pressure. Pharmacography and modality of administration: o Avaiable in oral: Tablet 100-200mg. Pharmacologic effects: The action on both α1 (relaxation of arterial smooth muscle and vasodilation) and β Rs (β1 blockade contributes to a fall in blood pressure in part by blocking reflex SY stimulation of the heart) contribute to the fall in blood pressure. congestive heart failure. This action decreases cardiac output. Therapeutic use: Used to treat mild to severe hypertension. It has a particular indication in the treatment of pregnancy-induced hypertension (pre-eclamsia) d. f. sol 100/200mg per 20/40ml vial For hypertensive emergencies. vascular and uterine) receptor sites. It reduces peripheral resistance while preventing reflex tachycardia. Adverse effects: it can cause postural hypotension and jaundice. 1 per 24h for 30 days . 100mg Nr. e. Pharmacological class: sympathetic antagonist b. bradycardia.XXX D. 8. RP/ Dg/Chronic Hypertension Rp/Labetalol tab. contraindications: asthma. Mechanism of action: non-selective beta-blocker with alfa1 blocking activity. for therapy of chronic hypertension.s. orally. Labetolol blocks stimulation of beta1-adrenergic (myocardial) and beta2-adrenergic (pulmonary. any degree of heart block.

slows heart rate and reduces blood pressure e) Pharmacography and modality of administration:  Oral: tablet. RP/ Dg/Glaucoma Rp/Timolol ophthalmic sol.It reduces aqueous humour production through blockage of the beta receptors on the ciliary epithelium and thus intraoqular pressure.5%. b) Mechanism of action: A non-selective beta blocker. conjuctivally 2 drops in each conjuctival sac for 10 days .confusion.10mg  Ophthalmic: liquid. slows heart rate and reduces blood pressure (depresses renin secretion). solution drops f) Adverse effects: The most serious possible side effects include cardiacarrhythmias and severe bronchospasms. To treat glaucoma to prevent heart attacks to prevent migraine headaches to treat high intraoqular pressure d) Pharmacologic effects: .s. c) Therapeutic use:      to treat high blood pressure. depression.25%-0. Also Decreases cardiac output. 0. Timolol can also lead to fainting. congestive heart failure.a) Pharmacological class: Sympathetic antagonist. worsening of Raynaud's syndrome and impotence. blocks stimulation of beta1- adrenergic (myocardial) and beta2-adrenergic (pulmonary.I D.25% Nr. vascular and uterine) receptor sites. This action decreases cardiac output. solution 0. g) Contraindications: o caution if peripheral vascular dz o caution if bronchospastic dz o caution if major surgery o caution if diabetes mellitus o caution if thyroid disorder o caution if WPW syndrome o caution if pheochromocytoma o caution if renal impairment o caution if hepatic impairment o caution if pregnancy 2nd or 3rd trimester o caution if myasthenia gravis 8.

ointment. d) Pharmacologic effects: Its general actions last about 4 hours except when placed topically in the eye. g ) Contraindications: glaucoma. Instill 1 drop in each conjuctival sac for 7 days . delirium. acute angle-closure obstructive uropathy paralytic ileus toxic megacolon asthma myasthenia gravis caution in elderly pts caution if high environmental temperature 8. sweat and lacrimal glands. tablet  Intramuscular injection.  Antisecretory: blocks secretions in upper and lower respiratory tracts prior to surgery. antimuscarinic agent. f) Adverse effects:  Dry mouth.  Oral: liquid. confusion. Cardiovascular: depending on the dose: ◦ low doses: bradycardia ◦ higher doses: the cardiac rate increases modestly. solution/drops.  Antidote for cholinergic agonists: used for treatment of overdoses of insecticides. preventing acetylcholine from binding to those sites.  Intravenous injection. Eye: persistent mydriasis.     e) Pharmacography and modality of administration:  Ophthalmic: liquid. constipation. where it binds competitively. unresponseviness to light. b) Mechanism of action:Has a high affinity for muscarinic receptors. Urinary system: reduces hypermotility states of urinary bladder. hallucinations.  Antisecretory: blocks salivary.a) Pharmacological class: Cholinergic antagonist. solution. where the action may last for days. depression. tachycardia.  CNS: restlessness. blurred vision.s. Atropine acts both centrally and peripherally. RP/ Dg/Uveitis Rp/Atropine ophth sol 1% Nr. Gastrointestinal: reduces activity of GIT.  Antispasmodic: relax GIT and bladder.  Collapse of circulatory and respiratory system. c) Therapeutic use:Ophthalmic: permits measurement of refractive errors without the interference of accomodative capacity of the eye.I D.

s.  Oral: liquid. RP/ Dg/Glaucoma Rp/Pilocarpine ophth. e) Pharmacography and modality of administration:  Ophthalmic: gel.a) Pharmacological class: direct acting cholinergic agonists b) Mechanism of action: Cholinergic parasympathomimetic agent that stimulates muscarinic receptors.I D. tears. saliva. conjuctivally 2 drops in each conjuctival sac for 30 days . d) Pharmacologic effects: o topically in cornea:  miosis and spasms of accomodation of eye.  Impossibility to foccus vision. Hepatic impairment. It stimulates profuse sweating and salivation. solution. drops. liquid. increasing secretion by the exocrine glands. Respiratory diesases. g) Contraindications:     cardiovascular diseases. f) Adverse effects: Pilocarpine can enter the brain and cause CNS disturbances.  Increased drainage of aqueous humor. c) Therapeutic use: Use in both narrow angle and wide angle glaucoma. tablet. 8. and producing contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes). Psychiatric disorder. Sol 1% Nr. o Secretory: stimulation of sweat. solution.

RP/ Dg/ Myasthenia gravis Rp/Neostigmine tab. a reversible cholinesterase inhibitor. 15mg Nr.XXX D. nausea. e) Pharmacography and modality of administration:  Intramuscular: liquid. neostigmine indirectly stimulates both nicotinic and muscarinic receptors which are involved in muscle contraction.  Intravenous: liquid. g) Contraindications: Contraindicated in patients with known hypersensitivity to the drug. abdominal pain.. c) Therapeutic use: used in symptomatic treatment of myasthenia gravis. diarrhea and bronchospasm. decreased blood pressure. orally 2 tabs per day for 15 days .s.  Used to stimulate bladder and GIT.  Oral: tablet.a) Pharmacological class: Indirect-acting cholinergic agonists. The drug inhibits acetylcholinesterase which is responsible for the degredation of acetylcholine. d) Pharmacologic effects:  reversibly inhibits acetylcholinesterase. flushing. with acetylcholinesterase inhibited. It does not cross the blood-brain barrier. specifically.  Used as an antidote for tubocurarine and other competitive neuromuscular blocking agents. b) Mechanism of action: Neostigmine is a parasympathomimetic. So. 8.  Stimulates contractility of skeletal muscle.15mg f) Adverse effects:salivation. more acetylcholine is present By interfering with the breakdown of acetylcholine. patients with peritonitis or mechanical obstruction of the intestinal or urinary tract.

blurred vision. bitter taste.s. c) Therapeutic use:     Treatment of peptic ulcer. decreased sexual ability or desire. 30 mins before food . Prophylaxis of duodenal ulcer recurrence. intestines and bladder. e) Pharmacography and modality of administration:  Tablets 25mg f) Adverse effects: Dry mouth.a) Pharmacological class: Antimuscarinic agent. d) Pharmacologic effects:  It reduces gastric acid secretion. nausea or loss of appetite. Prevents nausea. dizziness. b) Mechanism of action: Muscarinic receptor antagonist that binds to the muscarinic acetylcholine receptor. LX D. orally 1 tab per 24h for 30days. gastric ulcer and duodenal ulcer. diarrhea. RP/ Dg/Peptic ulcer Rp/Pirenzepine tab 25mg Nr.  It reduces muscular spasms. vomiting and motion sickness. drowsiness. bad breath g) Contraindications: Renal failure 8. Relieves cramps or spasms of the stomach. constipation.

acute angle-closure glaucoma. nausea. Also. inhibiting bronchoconstriction and mucus secretion. Hypersensitivity to atropine and related substances.s. Most likely due to actions of cGMP on intracellular calcium. tachycardia.a) Pharmacological class : nonselective muscarinic antagonist b) Mechanism of Action : Ipratropium bromide is an anticholinergic agent. The inhalation itself can cause headache and irritation of the throat in a few percent of patients. caution may be warranted. especially by in men with prostatic hypertrophy. g) Pharmacography : Nasal Spay or aerosol. resulting in a decrease in the formation of cyclic guanosine monophosphate (cGMP). e) Contraindications : narrow angle glaucoma and obstructions in the gastrointestinal tract and urinary system f) Adverse Effects : Dry mouth and sedation have been reported. respiratory solution h) Prescription Dg/Asthma Rp/IPRATROPIUM BROMIDE MDI 18µg Nr. Inhaled ipratropium does not decrease mucociliary clearance. without specificity for subtypes. I D. d) Therapeutic uses (indications) : For maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease. palpitations and headache have been observed. effects such as skin flushing. inhalatory 1 puff 3 times per day for 14days . As a result. c) Pharmacologic effects : Decreased contractility of smooth muscle in the lung. this results in decreased contractility of smooth muscle. It blocks muscarinic cholinergic receptors. including chronic bronchitis and emphysema. Urinary retention has been reported in patients receiving doses by nebulizer.