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Biochemistry of Emergency Drugs

Miss Yah Nee Lo Lecturer
Friday, August 26, 2011

Learning Objectives
• Know the common classes of drugs used in the A&E especially in Brunei • Be able to describe the mechanism of action of important classes of emergency drugs • The basic dosage and infusion guide of emergency drugs?
Friday, August 26, 2011

Accident & Emergency situations
• List down the common situations or conditions that comes into our own A&E department in the RIPAS that you can think of? • Shortness of breath • Anaphylactic shock • Cardiovascular problem e.g. heart block, arrhythymia, etc • Heart Attack …

Friday, August 26, 2011

August 26.Asthmatic/ COPD Friday. 2011 .

• MOA unclear Friday.1. Aminophylline • Bronchodilator • Compound of the bronchodilator theophylline with ethylenediamine in 2:1 ratio • Ethylenediamine improves solubility • Theophylline relaxes bronchial smooth muscles. 2011 . August 26.

2011 . August 26. diarrhoea. avoid bolus dose if patient taking Oral Theophylline • Adverse Drug Effects: Nausea. headache. • the potentially fatal: Convulsions. Vomiting.Aminophylline • contradictions: hypersensitive. hypotension and sudden death after too rapid IV injecion •Loading dose: 250 mg (Slow I/V in 15 mins) •Infusion Rate: 20-80 mils/hr 6 Friday. abdominal pain.. dizziness.. insomnia. cardiac arrthymias.

August 26. levelbuterol and s-albuterol. Salbutamol • Short acting B2-adrenergic receptor agonist used for relief of bronchospasm • racemic mixture with a 1:1 ratio of the isomer.2. 2011 . • The tertiary butyl group in sulbutamol makes it more selective for B2-receptors. Friday.

2011 . anticonvulsants • Indications: • • • • Seizures of eclampsia TDP Hypomagnesaemia Refractory VF Use with caution in renal failure • CNS depressant effects may be enhanced in presence of other CNS depressant • Friday.3. Magnesium Sulphate • sterile solution of magnesium sulphate heptahydrate in water for injection • Electrolyte. August 26.

2011 9 . constricts blood vessels. prepare us for ‘fight-or-flight’ response of the sympathetic nervous system. phenylalanine and tyrosine • used best for anaphylactic shock Friday.Adrenaline • Sympathomimetic • hormone and a neurotransmitter • increases heart rate. • Chemically it is a catecholamine.a. August 26. a monoamine produced only by the adrenal glands from the a.

2011 . August 26.Doxapram (Dopram) • Doxapram hydrochloride • Central Respiratory stimulant • Stimulates increase in tidal volume and RR • Stimulates the chemoreceptors in the carotid arteries which in turn stimulates the respiratory centre in the brain • Thought to stimulate the carotid body by inhibiting certain potassium channels 10 Friday.

2011 .Bradycardia & Heart Block Friday. August 26.

August 26. restlessness. 2011 .1. • abolishes bradycardia and reduces heart block due to vagal activity • Adverse reaction: Dry mouth. contipation. etc 12 Friday. Dysphagia. bronchial muscles. Atropine • MOA: Anticholinergic agent that competitively blocks the muscarinic receptors • Muscarinic receptors found in peripheral tissues such as the heart. confusion. iris and secretory glands. intestines.

2011 .2. Isoprenaline • MOA: a beta-1 and beta-2 adrenergic receptor agonist. 13 Friday. August 26.

August 26. 2011 .Antiarrythmics Friday. effect on action potential or on repolarization. flecainide 15 • Class II. August 26. lignocaine. shorten QT.g.disopryamide • Class 1b. prolong PR.Membrane stabilizers • Class Ia. prolong repolarization. QRS. procainamide. mexilitine. raise fibrillation threshold e.shorten action potential. Quinidine.g. shorten repolarisation. phenytoin • Class 1c. propanolol Friday. QT.g.lengthen action potential. 2011 .beta blockers e.Classes of antiarrythmics • Class 1. prolongs PR and QRS e. e.

Potassium channel blockers that prolong duration of action potential e. amiodarone. disopryamide • Class IV. Verapamil Friday.Classes of antiarrythmics • Class III. 2011 16 .g. e. August 26.Calcium channel blockers that have important effects on upper and middle parts of the AV node.g.

Adenosine (Adenocor) • Purine Nucleoside • comprise of a molecule of adenine attached to a ribose sugar molecule via a β-N9 glycosidic bond. August 26. 2011 . causes transient heart block in the AV node • Via A1 receptor. • also acts as a neurotransmitter • when administered I.. reducing cAMP and so causing cell hyperpolarization by increasing outward potassium ion flux 17 15 Friday. inhibiting adenylyl cyclase.1.V.

Lignocaine • Class 1B antiarrythmic drug • also act as local anaesthetic.2. • contain amide group in the structure • MOA: block the fast voltage gated sodium (Na+) channels • inhibit sodium influx • block rise of action potential • inhibit signal conduction Friday. 2011 18 16 . August 26.

dilates the main coronary arteries and arterioles both in normal and ischemic regions.3. Verapamil • MOA.Calcium ion influx inhibitor • L-type calcium channel blocker • relaxation and prevention of coronary artery spasm. August 26. 2011 19 17 . Friday.

amiodarone 20 18 Friday. Amiodarone • Class III antiarrthymic drug • Blocks sodium channels at rapid pacing frequencies • noncompetitive antisymphatetic action • lengthen cardiac action potential • negative chronotropic effect in nodal tissues • blocks myocardial potassium channels --> contributes to slowing of conduction and prolongation of refractoriness in the AV node. August 26. • hypotension is the most common adverse effect seen with I. 2011 .V.4.

in cardiac cells Disopyramide Procainenamide 21 Friday.Procainamide & Disopyramide • Both are Class 1a antiarrythmics • interfere directly with the depolarization of the cardiac membrane • Inhibits the fast sodium channels • Increases the duration of a. 2011 . August 26.p.

2011 22 . August 26. R(+) and S (-) Friday.Propanolol • A synthetic non selective beta-adrenergic receptor-blocking agent. • arrhythmia and thyroid crisis as well as hypertension • blocks action of the sympathetic nervous system by blocking beta receptors on sympathetic nerves • highly lipophilic • undergoes high first pass metabolism by the liver • only about 25% reaches systemic circulation • racemic mixture of two enantiomers.

August 26. • blocks action of the sympathetic nervous system by blocking beta receptors on sympathetic nerves • also reduces force of contraction of the heart Friday.Metoprolol • Beta-adrenergic blocking agent • use also for hypertension. heart pain • similar to propanolol. 2011 23 .

2011 . August 26.Hypertensive crisis Friday.

limiting release of calcium from SR of smooth muscle. 2011 25 . lower bp.Hydralazine (Apresoline) • Direct-acting smooth muscle relaxant • vasodilator primarily in arteries and arterioles.1. August 26. • MOA: increase guanosine monophosphate (GMP) decreasing action of second messenger IP3. reduce peripheral resistance. Friday. • Relaxing vascular smooth muscle.

R) isomer is a mixed nonselective beta blocker and selective alpha 1 blocker • the ratio of alpha:beta block is apporoximately 3:1 • • • • • Friday.S)-isomers are inactive.R)-isomer is a powerful alpha one blocker • the fourth (R. August 26.2. • the third (S. Labetalol mixed alpha/beta adrenergic antagonist acute hypertension and hypertensive crisis has stereoisomers is a racemic mixtures of four isomers. 2011 26 . Two of these the (S.and (R.S).

August 26.Vasoactive Drugs Friday. 2011 .

August 26. Dopamine • also act as a catecholamine neurotransmitter in the brain • intravenous medication acting on sympathetic nervous system • precursor for noradrenaline and releases it from intracardiac adrenergic nerve endings. • in the periphery. • effects like increased heart rate and blood pressure Friday. 2011 28 .1. dopamine stimulates prejunctional dopaminergic DA2-receptors which results in inhibition of NA release and inturns. facilitates vasodilation.

• Clinically used to treat acute but potentially reversible heard failure • acts on the beta1 receptors of the heart to reduce its contractility and cardiac output. August 26. 2011 29 . Dobutamine • Sympathomimetic Drug for treatment of heart failure and cardiogenic shock • Direct stimulation of beta-one receptors of the sympathetic nervous system. • * Since it does not induce release of NA like DOPAMINE. it is less prone to induce hypertension Friday.2.

2011 30 .3. August 26. Noradrenaline • also a hormone and a neurotransmitter • Potent alpha agonist with some beta-adrenergic properties • shown to increase MAP in patients with hypotension resistant to fluid resuscitation in patients with septic shock Friday.

Quiz time Text Friday. August 26. 2011 .

Myocardial Infarction Friday. August 26. 2011 .

although none can activate plasminogen independently • Extra streptokinase --> extra plasmin production --> break down of fibrin --> dissolve clots • given IV ASAP after onset of MI to dissolve clots in ther heart arteries.1. and γ (residues 288–414). Streptokinase Protein secreted by streptococci Effective thrombolysis medication. Each domain binds plasminogen. • Note the difference in dosage for patients coming in for MI or PE • • • • Friday. MI. 2011 33 . August 26. β (residues 151–287). denoted α (residues 1–150). Fibrinolytics There are three domains to Streptokinase. PE.

Nitroprusside • Inorganic compound with formula Na2[Fe(CN)5NO].2. • Once in the circulation. 2H2O • Red Coloured Salt. • Good for Heart Failure + Malignant Hypertension 34 Friday.potent Vasodilator in arterioles (more) and venules. • Complex anion with an octahedral ferrous center surrounded by 5 tightly bound cyanide ligands and a linear nitric oxide ligand. it break downs to release NO --> activates guanylate cyclase in smooth muscle and increase cGMP --> stimulate Ca2+ to ER and reduce availibility--> relaxation of smooth muscles --> vessels dilate. August 26. 2011 .

Eclampsia .Magnesium Sulphate Friday. 2011 . August 26.

August 26.Status Epilepticus Friday. 2011 .

2011 37 . August 26. Phenytoin • Chemical structure related to barbiturates • Antiepiletic • Stabilize the inactive state of voltage gated sodium channels • Suppress abnormal brain activity seen in seizures ---> by reducing the electrical conductance among brain cells Friday.1.

alchohol withdrawal. Diazepam • Benzodiazepine group • Commonly for anxiety. • MOA: enhances the effect of neurotransmitter GABA by binding to the benzodiazepine site on the GABA A receptor leading to CNS depression • GABA A receptor activated ---> increase in chloride ions influx into cell ---> increased hyperpolarisation --> hard to achieve ation potential --> reduce in excitation Friday. 2011 38 . muscle spasm and of course seizure including status epilepticus. August 26. insomnia.2.