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MEDICINAL CHEMISTRY
YASH GARG ques. and drugs unit - 2 according to Pharmacy council of india
| Question | Answer |
|---|---|
| what is mao | monoamine oxidase is a enzyme and a drug target to treat neuropsychiatric disorders the biological importance of mao is to regulate amine levels in brain and metabolize amine and drugs in the periphery |
| how many drugs are direct acting | 14 drugs nor epinephrine , epinephrine , phenyephrine , dopamine , methyldopa, clonidine, dobutamine , isoproterenol , terbutaline , salbutamol , bitolterol , naphazoline , oxymetazoline , xylometazoline |
| how many drugs are indirect acting | 3 hydroxyamphetamine , pseudoephedrine , propylhexedrine |
| how many drugs are mixed acting | 2 ephedrine , metaraminol |
| mechanism of action of nor epinephrine | potent at alpha receptor less than adrenaline also effect on beta 1 receptor but not on beta 2 |
| what are prodrug with example | inactive outside but active after crossing first pass effect used to prevent first pass effect example epinephrine |
| which drug is potent for all receptors | epinephrine |
| on acetylation of phenol with 2-chloro acetyl chloride gives ? | m-chloroacetylphenol |
| on reacting m-chloroacetylphenol with methylamine gives ? | 1-(3-hydroxyphenyl)2-(methylamino)ethanone |
| on reduction of 1-(3-hydroxyphenyl)2-(methylamino)ethanone gives ? | phenylephrine |
| on which receptor does phenylephrine attaches and give effect ? | alpha 1 but no action on beta |
| what is dopamine | it is a neurotransmitter that helps to regulate movement and emotional responses also for feeling of pleasure |
| at which receptor dopamine binds ? | directly on beta indirectly on alpha |
| Moa of methyldopa | methyldopa is converted into alpha methyl nor epinephrine by enzyme dopamine beta hydroxylase and bind with alpha2 receptor |
| in which receptor clonidine binds ? | alpha 2 |
| dobutamine binds with ? | beta 1 and alpha 1 directly |
| which drug increse cardiac output when bind on beta 1 | isoproterenol |
| which drug increase bronchodilation when bind on beta 2 | isoproterenol (isoprenaline) |
| terbutaline bind with which receptor | beta 2 |
| salbutamol bind with which receptor | beta 2 directly |
| on acetylation of phenol with 2-chloro acetyl chloride gives ? | m-chloroacetylphenol |
| on reacting m-chloroacetylphenol with methylamine gives ? | 1-(3-hydroxyphenyl)2-(methylamino)ethanone |
| on reduction of 1-(3-hydroxyphenyl)2-(methylamino)ethanone gives ? | phenylephrine |
| on which receptor does phenylephrine attaches and give effect ? | alpha 1 but no action on beta |
| what is dopamine | it is a neurotransmitter that helps to regulate movement and emotional responses also for feeling of pleasure |
| at which receptor dopamine binds ? | directly on beta indirectly on alpha |
| Moa of methyldopa | methyldopa is converted into alpha methyl nor epinephrine by enzyme dopamine beta hydroxylase and bind with alpha2 receptor |
| in which receptor clonidine binds ? | alpha 2 |
| dobutamine binds with ? | beta 1 and alpha 1 directly |
| which drug increse cardiac output when bind on beta 1 | isoproterenol |
| which drug increase bronchodilation when bind on beta 2 | isoproterenol (isoprenaline) |
| terbutaline bind with which receptor | beta 2 |
| salbutamol bind with which receptor | beta 2 directly |
| on acetylation of 2-hydroxy benzyl alcohol with 2-chloro acetyl chloride gives ? | 5-acetylchloride-2-hydroxybenzylalcohol |
| 5-acetylchloride-2-hydroxybenzylalcohol on reacting this with 2-methylpropan-2-amine gives ? | salbutamon |
| on reducing salbutamon gives ? | salbutamol |
| bitolterol binds with which receptor and is a prodrug of | beta 2 ; colterol |
| which drug is a powerful alpha receptor | naphazoline |
| which drug is the partially agonist of alpha 1 and selective agonist of alpha 2 | oxymetazoline |
| MAO of xylometazoline | it binds on both alpha 1&2 receptors |
| what are indirect acting drugs | these drugs do not themselves react with receptor but causes release of neurotransmitter from storage sites which then interacts with receptors to produce effects |
| what are direct acting drugs | these are those drugs which directly binds with adrenergic receptors both (alpha and beta ) and give its pharmacological action |
| MOA of hydroxyamphetamine | cause release of nor adrenaline from nerve synapse and causes dilation of pupil |
| pseudoephedrine MOA | stimulates both alpha and beta receptors and stimulates cns |
| propylhexedrine MOA | activates alpha receptor in the mucosa of respiratory tract works same as nor epinephrine and epinephrine |
| what is agonist | A drug or substance that binds to a receptor inside a cell or on its surface and causes the same action as the substance that normally binds to the receptor. |
| what is antagonist | a drug that binds to the receptor either on the primary site, or on another site, which all together stops the receptor from producing a response |
| what is agents with mixed action mean ? | these are those drugs which directly act on adrenergic receptors and also effect the release of noradrenaline act as both direct or indirect acting drugs |
| from which medicinal plant ephedrine occurs | ephedra |
| how many optical isomers are present of ephedrine | 4 (-)ephedrine & (+) ,(-)pseudoephedrine & (+) |
| MOA of ephedrine | stimulates bot alpha and beta also effect cns stimulation |
| metaraminol acts on receptors ? | both alpha and beta and stimulate noradrenaline |
| uses of nor epinephrine | strong vasoconstriction treatment of hypotension localize effect of local anesthetics |
| uses of epinephrine | vasoconstriction , treatment of asthma relaxes bronchial muscles emergency treatment of anaphylaxis and anaphylactic shock in the cardiopulmonary disease |
| phenylephrine uses | vasoconstriction hypotension mydriatic agent during eye surgery |
| what is mydriatic | prolonged dilation of pupil of eye |
| uses of dopamine | shock patient ; congestive heart failure by increasing bp and urine out flow ; in trauma septic shock |
| uses of methyldopa | antihypertensive ; REDUCE HIGH BP |
| uses of clonidine | hypertension ; mild sedative |
| uses of dobutamine | treat heart failure during cardiac surgery ; treat conjestive heart failure |
| uses of isoproterenol (isoprenaline) | treat bronchial asthma ; bradycardia |
| uses of terbutaline | orally given to treat asthma ; also used as an aerosol / inhalation |
| uses of salbutamol | used to relax uterine smooth muscles ; to delay premature labour ; relief of bronchospasm |
| what is bronchospasm | narrowing of bronchi |
| uses of bitolterol | to treat asthma (bronchodilator) |
| uses of naphazoline | vasoconstrictor ; reduce swelling ; relief of rhinitis and sinusitis |
| what is rhinitis | inflammation of the mucosa membrane of nose or when a reaction occurs that causes nasal congestion, runny nose, sneezing, and itching due to any virus infection (common cold) or any allergic reaction |
| what is sinusitis | an inflammation or swelling of the tissue lining the sinuses |
| uses of oxymetazoline | due to vasoconstriction properties used to treat nose bleeding ; redness of eye due to irritation |
| uses of xylometazoline | constrictions of large veins in the nose ; treat symptoms of nasal congestion , allergies etc. |
| uses of amphetamine | eye drop to dilate pupil ; used as a diagnostic agents for testing horner's syndrome |
| what is horner's syndrome | Decreased eye pupil size, Horner syndrome is a condition that affects the face and eye on one side of the body. It is caused by the disruption of a nerve pathway from the brain to the head and neck |
| uses of pseudoephedrine | increase bp by increasing cardiac output and by causing vasoconstriction |
| uses of propylhexedrine | used for relief of congestion due to cold, allergies, rhinitis |
| uses of ephedrine | nasal decongestant ; used in various allergic disease like hay fever and urticaria |
| what is urticaria | a rash of round, red welts on the skin that itch intensely, sometimes with dangerous swelling, caused by an allergic reaction, typically to specific foods |
| uses of metaraminol | to treat hypotension |
| what are adrenergic antagonist | these are those agents or drugs which inhibit the effect of sympathomimetic agents by blocking the receptor |
| how many alpha antagonist drugs are present | 6 tolazoline ; phentolazoline ; phenoxybenzamine ; prazosin ; dihydroergotamine ; methysergide |
| tolazoline | competitive inhibitor of alpha R ; belong to non-selective alpha adrenergic blockers |
| moa of tolazoline | it is structurally same as alpha agonist so they blocks the alpha receptor and stop the alpha agonist to produce effects |
| uses of tolazoline | vasodilator ; stimulate gastric secretion ; antagonize the overdose of clonidine |
| when benzyl cyanide react with ethylene diamene in the presence of carbon disulfide gives ? | tolazoline |
| uses of phentolamine | it is non selective (blocks both 1&2) vasodilators ; control hypertension conditions |
| uses of phenoxybenzamine | it is non selective (blocks both 1&2) ; treat urinary retention ; hypertension caused by phaeochromocytoma |
| what is phaeochromocytoma | a small vascular tumour of the adrenal medulla, causing irregular secretion of adrenalin and noradrenaline leading to attacks of raised blood pressure, palpitations, and headache |
| uses of prazosin | it is selective alpha 1 drug ; used to treat heart failure , raynaud's syndrome |
| uses of dihydroergotamine | bocks both 1&2 alpha ; treat migraine ; medication overdose headache ; vasoconstrictor |
| uses of methysergide | it is a potent serotonin antagonist works on both alpha 1&2 ; used as prophylactic in the treatment of severe recurrent migraine |
| how many beta adrenergic blockers are there ? | 9 propranolol ; metibranolol ; atenolol ; betazolol ; bisoprolol ; esmolol ; metoprolol ; labetolol ; carvedilol |
| moa of propranolol | it is non cardioselective beta adrenergic blockers ; moa is due to decrease renin release or reduced cardiac output |
| uses of propranolol | treat hypertension ; cardiac arrhythmia |
| when alpha naphthol is treated with epichlorohydrin in the presence of base , the intermediate formed is then treated with isopropylamine gives ? | propranolol |
| epichlorohydrin consist of | 1 epoxy group and one chloro at the end of propyl chain |
| uses of metibranolol | non selective ; treat glaucoma |
| uses of atenolol | beta 1 selective ; antihypertensive ; treat cardiac arrhythmia |
| uses of betazolol | beta 1 selective ; treat hypertension ; heart failure |
| moa of labetolol | non selective beta blocker but act as a competitive blocker on both alpha 1 and beta receptor |
| uses of labetolol | treat hypertension |
| moa of carvedilol | non selective beta blocker and competitive alpha 1 due to alpha 1 blockage it relaxes blood vessels , dilates them and lower blood pressure |
| uses of carvedilol | antihypertensive ; congestive heart failure |
| what are common catecholamine ? | dopamine ; nor-epinephrine ; epinephrine |
| catecholamine consist of ? | 1catechol ring (2-hydroxyphenol) ; 1 ethylamine at 5th position |
| biosynthesis of catecholamine ? | phenylalanine(1-amino-2-phenylethanoicacid)>hydroxylase>tyrosine (1-amino-2-(3-hydroxyphenyl)ethanoic acid)>hydroxylase>DOPA(3,4-dihydroxyphenylalanine)>decarboxylase>dopamine>beta hydroxylase>nor-epinephrine>n-methyltransferase>epinephrine |
| where phenylalanine get hydrolase and to became what? | liver ; tyrosine |
| where tyrosine get hydrolyzed and to become what ? | cytoplasm of neurons ; DOPA |
| where DOPA get decarboxylate to produce which catecholamine ? | cytoplasm of neuron ; dopamine |
| where the nor-epinephrine get converted to produce which catecholmine ? | adrenal medulla ; epinephrine |
| by which enzyme dopamine get converted into nor-adrenaline ? | dopamine beta hydroxylase |
| by which enzyme nor-adrenaline get converted into adrenaline ? | phenylethanolamine-N-methyl transferase(PNMT) |
| by which two enzymes the catabolism of catecholamines is done ? | MAO ; COMT |
| MAO stands for ? | Monoamine oxidase |
| COMT stands for ? | catechol o-methyl transferase |
| mechanism of action of MAO is ? | deamination ; amine group is removed and aldehyde group is formed on attached last carbon to stop the action |
| mechanism of action of COMT ? | methylation on ring ; hydrogen of the meta hydroxy group is replaced with the methyl group to stop the action |
| alpha 1 is found in ? | post synaptic receptor sites ; smooth muscles ; liver ; excitatory in nature |
| alpha 2 is present in ? | pre and post synaptic receptor sites ; c.n.s ; pancreas ; inhibitory in nature |
| beta 1 is present in ? | cardiac tissue ; kidney ; excitatory in nature |
| beta 2 is present in ? | smooth muscles ; inhibitory in nature |
| SAR of sympathomimetic agents is done in _ ways ? | 3 ways ; 1. aromatic/catechol ring 2. carbon chain 3. amino group |
| how the SAR of aromatic/catechol ring of sym. agents is done ? | 1. hydroxy group at 3,4 position increase alpha beta potency absence decreases the potency ex. phenylephrine<epinephrine 2. but un-substituted ring easily cross BBB have more CNS activity ex. amphetamine |
| how the SAR of carbon chain of sym. agents is done ? | 1. beta carbon (C- next to ring) -OH group decreases the CNS activity but increase alpha beta activity ex. ephedrine 2. substitution on alpha carbon blocks metabolism results decrease activity of MAO and show longer action ex. amphetamine |
| how the SAR of amino group of sym. agents is done ? | 1.1* and 2* amino group have high alpha selectivity ex. epinephrine 2. more the size of alkyl substituent higher will be the beta selectivity action ex. salbutamol , isoprenaline |
| SAR of beta antagonists is done in _ ways ? | 3 ways ; 1. aromatic ring ,2. carbon chain ,3. amino group |
| how the SAR of aromatic ring of beta antagonist is done ? (phenyl ring is not napthyl ring) | 1. if alkenyl (-ch2ch=ch2) and alkenoxy (-och2ch=ch2) group is present on ortho position of phenyl ring give good beta antagonist activity ex. alprenolol and oxprenolol 2.addition of -OH group in phenyl ring leads to removal of antagonist activity |
| if napthyl ring of propranolol is replaced with phenyl ring than what happens ? | it will loses non-selectivity character ex. atenolol, betazolol is selective agent and propranolol is non-selective |
| how the SAR of carbon chain of beta antagonist is done ? | the (-och2) group present between the aromatic ring and ethanolamino side chain is essential for the activity (aryloxy propanolamines) if not present decrease activity |
| how the SAR of amino group of beta antagonist is done ? | if isopropyl and t-butyl group is present on amino group , then it provides nucleophilicity to amino group increase activity ex. atenolol, timolol |
Created by:
i.yashgarg
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