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* Do not miss the test on this topic on the TEST PACKAGES page. This blog prepares you for GPAT RRB Pharmacist Recruitment Exam Common Recruitment Examination for AIIMS Pharmacist KGMU Pharmacist Recruitment Exam KSSSCI Pharmacist Recruitment Exam MPESB Pharmacist Recruitment Exam Drugs Inspector Exams Drugs Controller Exams DPEE D.Pharm, B.Pharm, and Pharm.D. Exams • Atropine is a prototype anticholinergic/antimuscarinic/parasympatholytic drug. • It blocks the action of acetylcholine by blocking the muscarinic cholinergic receptors. • It does not block nicotinic cholinergic receptors. • It is a naturally occurring tropane alkaloid that is found in Atropa belladonna and Hyocyamus niger. • Atropine is a racemic mixture of l-hyoscyamine and d-hyoscyamine. • It occurs as colourless crystals or white crystalline powder. It is odourless and has bitter taste. • Atropine is official as sulphated salt which contains one molecule of water of crystallization. • Atropine has low solubility in water but its official salt, atropine sulphate is very soluble in water. • It is an amino alcohol ester. It is composed of a tropine (an amino alcohol) and a tropic acid (a carboxylic acid), which form an ester bond (see image). • In acidic or alkaline medium, it is hydrolyzed to give tropine and tropic acid. • Storage condition: It is required to be kept in well closed containers, protected from light. Pharmacological Actions of Atropine • Pharmacological actions of atropine are observed mainly because it competitively antagonizes acetylcholine at the muscarinic receptor. • Atropine doesn’t affect the nicotinic actions of acetylcholine at autonomic ganglia and skeletal muscles. • Effect on secretions: Atropine reduces the volume and total acidity of gastric secretions. It also reduces salivary secretion (salivary glands secretion), secretions in nose, pharynx, and bronchi. It also reduces the sweat secretion. • Effect on smooth muscles: Usually, atropine relaxes all smooth muscles such as that of gastrointestinal tract, urinary tract, bronchi, etc. • Atropine stops excessive tone and motility of gastrointestinal tract. It does not interfere with normal peristalsis. • Atropine reduces normal as well as drug induced ureteral peristalsis. It reduces tone of bladder muscles and tends to produce urinary retention. • Atropine is effective in relieving the bronchospasm produced by cholinergic drugs. • Effect on eye: On local instillation, atropine produces mydriasis by blocking the cholinergic nerve supply. It causes photophobia and ‘Paralysis of accommodation’ that is known as ‘Cycloplegia’. • Effect on cardiovascular system: Atropine in therapeutic doses may initially decrease the heart rate because it has partial agonist property with acetylcholine. But it is followed by tachycardia. Toxic doses of atropine produce cutaneous vasodilation resulting in atropine flush and hypotension. • Effect on CNS: Atropine in therapeutic doses stimulates the medullary vagal nuclei. This causes increase in rate and depth of respiration. At low doses, it causes slight restlessness; and at high or toxic doses it causes restlessness, agitation, hallucination. Important Dosage, Indications and Contraindications of Atropine • Bradycardia: 1 mg every 3 to 5 minutes upto a max. total dose of 3 mg I.V. (Adult). Repeat the doses until obtaining the desired effects. • As preanaesthetic agent: 2 mg oral/0.2 to 1 mg I.V., I.M., or S.C. 30 to 60 min prior to anesthesia. • Antisialogogue/Antivagal: 0.5 mg to 1 mg every 1 to 2 hours I.V. (Adult) • Organophosphate/Muscarinic poisoning: 2 to 3 mg every 20 to 30 min I.V. (Adult) • Irritable bowel syndrome, non-ulcer dyspepsia and diverticular disease: Adult: 0.6 to 1.2 mg as a single dose at bed time. • Ophthalmic: Uveitis, iritis: 1% solution: Instill 1-2 drop(s) into the eye up to 4 times daily (adults). • Contraindications: Glaucoma, Benign prostatic hyperplasia, achalasia of esophagus, paralytic ileus, severe ulcerative colitis, intestinal ileus, severe ulcerative colitis, intestinal atony, obstructive uropathy, myasthenia gravis, CHF with tachycardia. Atropine Brand names: Atro Injection, Atrosulph, Atropine. Atropine Poisoning/ Belladonna Poisoning Atropine/ belladonna poisoning may occur due to drug overdose or consumption of seeds and berries of belladonna/datura plant. Symptoms of poisoning are: Dry mouth, difficulty in swallowing and talking, dry, flushed and hot skin, fever, urinary retention, decreased bowel sounds, a scarlet rash may appear, dilated pupil (mydriasis), photophobia, blurring of near vision, hypotension, weak and rapid pulse. The central effects include restlessness, confusion, psychotic behaviour, weakness, muscle in-coordination, hallucinations, convulsions, and coma. Finally cardiovascular collapse with respiratory depression and failure. Treatment Treatment should be started in a dark quiet room to relieve photophobia. Treatment includes gastric lavage, universal antidote, anticholinesterase such as physostigmine / neostigmine and other general measures such appropriate. MCQs 1. Which one of the following is not the therapeutic use of atropine? (a) As a mydriatic (b) As an antidote for organophosphate poisoning (c) As a preanaesthetic medication (d) As an anti-inflammatory agent 2. Atropine sulphate, a parasympatholytic drug belongs to the class _____. (a) Amino alcohol esters (b) Amino alkyl ethers (c) Amino alcohols (d) Amino amides To proceed with the TEST ON ATROPINE,
* Do not miss the test on this topic on the TEST PACKAGES page. This blog prepares you for GPAT RRB Pharmacist Recruitment Exam Common Recruitment Examination for AIIMS Pharmacist KGMU Pharmacist Recruitment Exam KSSSCI Pharmacist Recruitment Exam MPESB Pharmacist Recruitment Exam Drugs Inspector Exams Drugs Controller Exams DPEE D.Pharm, B.Pharm, and Pharm.D. Exams Cholinergic Receptors: • The receptors which respond to Acetylcholine are cholinergic receptors. These receptors are found in central and peripheral nervous system. • There are two main types of cholinergic receptors: Nicotinic and Muscarinic receptors. Nicotinic Receptors • Nicotinic receptors are directly linked to ligand gated ion channels. • They are selectively activated by nicotine and blocked by tubocurarine or hexamethonium. • On the basis of location and selectivity, nicotinic receptors are divided into two types; I) N1 or Nm: These receptors are present at skeletal muscle endplate and mediate skeletal muscle contractions. They are selectively stimulated by phenyltrimethyl ammonium and are blocked by tubocurarine. II) N2 or Nn: These are present in ganglionic cells, adrenal medullary cells, in spinal cord and in certain areas of brain. In CNS Ach plays a significant role in memory, arousal and analgesia through Nn receptors. Muscarinic Receptors • The Muscarinic receptors are named such because they are responsive to muscarine (a natural alkaloid). • Muscarinic receptors are metabotropic i.e. G-protein coupled receptors. • There are five types of Muscarinic receptors: M1, M2, M3, M4 and M5. M1 Receptors: o M1 is Gq protein - coupled receptor. o It has + ve effect. It stimulates the target organ. o M1 is generally found in two specific locations: CNS where it is involved in memory, arousal and analgesia and parietal cells (gastric glands) where it increases the stomach acid. o It also increases endocrine gland secretions such as increase in the saliva. o M1 receptors work via phospholipase C, increasing IP3 and DAG levels. M2 Receptors: o M2 receptors are cardiac muscarinic receptors. o M2 receptors are Gi protein - coupled receptors. o They have –ve effect. o They are inhibitory; hyperpolarizing membranes by increasing potassium conductance.M2 is mainly going to target two different places: one is the heart (SA node, AV node and bundle of his) and the other is presynaptic membrane. o M2 receptor at presynaptic membrane inhibits the further release of Ach. o M2 receptors increase heart parasympathetic effects and there will be decrease in the chromotropy, inotropy and dromotropy of the heart. M3 Receptors: o M3 receptors are glandular muscarinic receptors o They are found on exocrine glands, smooth muscles, ciliary muscles and pupil of the eye. o M3 is Gq protein - coupled receptor. o It has + ve effect. M4 & M5 Receptors: o M4 and M5 receptors are predominantly found in the CNS. They play role in memory, arousal and analgesia. o M4 receptors act through Gi protein to inhibit adenylate cyclase. They also function by a direct regulatory action on K+ and Ca2+ion channels. When M4 receptors in tracheal smooth muscle stimulated, they inhibit the release of Ach same as that of M2 receptors do. o M5 receptors may regulate dopamine release at terminals within the striatum. • SAR of Ach reveals that a cationic ammonium group is essential for muscarinic as well as nicotinic receptor activities. • Acetylcholine (agonist) and atropine (antagonist) compete with each other at muscarinic receptors. MCQs 1. Identify a wrong statement about cholinergic receptors. a) These receptors respond to Acetylcholine. b) They are found in ANS only. c) Nicotinic receptors are directly linked to ligand gated ion channels. d) M2 receptors are cardiac muscarinic receptors. 2. All of the following statements about nicotinic receptors are correct, except: a) Nm receptors are present at skeletal muscle endplate. b) Nn receptors are present in ganglionic cells. c) Nicotinic receptors are selectively activated by hexamethonium. d) Nicotinic receptors are found in central and peripheral nervous system. To proceed with the TEST ON CHOLINERGIC RECEPTORS,
GPAT Preparation RRB Pharmacist Recruitment Exam Common Recruitment Examination AIIMS Pharmacist KGMU Pharmacist Recruitment Exam KSSSCI Pharmacist Recruitment Exam MPESB Pharmacist Recruitment Exam Drugs Inspector Exams Preparation Drugs Controller Exams Preparation DPEE D.Pharm, B.Pharm, and Pharm.D. notes • Acetylcholine is a neurotransmitter. • Acetylcholine plays a crucial role in both the central nervous system (CNS) and the peripheral nervous system (PNS). In the PNS, it functions in both the voluntary (somatic) and involuntary (autonomic) nervous systems. • Acetylcholine is synthesized locally in the cholinergic nerve endings. • In cholinergic cells, an acetyl group is transferred from acetyl-coenzyme A (CoA) to choline to synthesize Ach. This reaction is catalyzed by the enzyme choline acetyltransferase (ChAT). • Choline acetyltransferase (ChAT) is synthesized in the rough endoplasmic reticulum of all cholinergic cells. • Acetylcholine is an ester of acetic acid and choline. • Acetylcholine is hygroscopic in nature and is water soluble. • Storage condition: As it is hygroscopic in nature, it should be stored in air-tight dry container in a cool place. • SAR of Acetylcholine (Ach) (See image): 1) SAR of Ach reveals that a cationic ammonium group is essential for muscarinic as well as nicotinic receptor activities. 2) If one or more of the methyl groups on nitrogen atom are replaced by hydrogen or ethyl group, both muscarinic as well as nicotinic receptor activities are reduced. 3) Only compounds possessing a positive charge on the atom in the position of the nitrogen has appreciable muscarinic activity. 4) The muscarinic agonist should have an oxygen atom, preferably ester-like oxygen, capable of participating in a hydrogen bond. 5) There should be no more than five atoms between the nitrogen and the terminal hydrogen atom for maximal muscarinic potency. This rule is known as Ings rule of five. 6) When the methyl groups are replaced by three ethyl groups, the resulting compound is a cholinergic antagonist. • There are two main types of receptors for acetylcholine: Nicotinic and Muscarinic receptors. • Nicotinic receptors are ligand gated ion channels. • Muscarinic receptors are primarily referred to as G protein coupled receptors (GPCR). • Pharmacological Actions of Cholinergic Drugs: In general, pharmacological actions of cholinergic drugs are 1. Decrease in heart rate, force of contraction and electrical conductivity in heart i.e negative chronotropic, negative inotropic and negative dromotropic effects on the heart respectively. 2. Hypotension 3. Increase in gastric motility 4. Micturition (urinary bladder) 5. Increase salivary secretion 6. Increase bronchial secretions and cause bronchospasm 7. Increase sweating 8. Miosis and reduction in intraocular tension (eye) 9. Spasm of accommodation (eye) 10. In CNS Ach plays a significant role in memory, arousal and analgesia through Nn receptors. • Cholinesterase is the enzyme that metablises ACh. Cholinesterases are of two types: 1) True cholinesterase i.e. Acetylcholinesterase is found primarily in the blood on red blood cell membranes, in neuromuscular junctions, and in other neural synapses. 2) Pseudo-cholinesterases i.e. Butyrylcholinesterase is produced in the liver and found primarily in blood plasma. • Neuromuscular-blocking agents block the action of acetylcholine at the neuromuscular junction (NMJ), thereby causing paralysis of the affected skeletal muscles. These agents are Nicotinic receptor blockers. • According to Cholinergic hypothesis, Alzheimers disease (AD) is caused due to reduced synthesis of acetylcholine. • Ach is used to induce miosis during ocular surgery. It has limited therapeutic uses because a considerable amount of it is destroyed immediately by pseudo cholinesterases in plasma and by true cholinesterase at the site of receptors. • Miochol-E is a brand name of Ach. It is acetylcholine chloride intraocular solution used to constrict the pupil of the eye during cataract surgery or other types of eye surgery. MCQs 1) In acetylcholine, replacement of one or more of the methyl groups on nitrogen atom by hydrogen or ethyl group a) Increases both muscarinic and nicotinic activity b) Decreases both muscarinic and nicotinic activity c) Increases the muscarinic activity d) Increases the nicotinic activity 2) What is wrong about acetylcholine? (a) It is an ester of acetic acid and choline. (b) It has positively charge carbon in its structure. (c) It is hygroscopic in nature. (d) It is water soluble. 3) Effect of acetylcholine on heart is ______. (a) positive chronotropic (b) negative chronotropic (c) positive inotropic (d) positive dromotropic 4) Neuromuscular-blocking agents block the action of ______ at the neuromuscular junction. (a) acetylcholine (b) histamine (c) adrenaline (d) noradrenaline 5) Which neurotransmitter is significantly reduced in the brain of Alzheimers patient? a) Acetylcholine b) Serotonin c) Dopamine d) GABA To proceed with the TEST ON ACETYLCHOLINE for GPAT under the GPAT category,
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Thank you for a great course. Great presentation style with lots of opportunities to ask questions and talk about real life examples which all made for a really enjoyable and informative course." "This has more than met my expectations."
Most of key points are covered which are most useful as study point of view..for DPEE and other competative exam.
These classes explained all key concepts of the pharmacy syllabus and then had online MCQ practice tests for perfect practice and confidence. Now, I have no worries for pharmacy syllabus for any recruitment exam.
I passed my d.pharm just because your efforts and trust in me. Before joining your classes, I gave Pharmacology (S.Y. D.Pharm) exam four times but failed. Then I joined your classes, understood my mistakes and passed the exam. Thank you, Pharmalife Academy.
These online pharmacology tutorials made my concepts of pharmacology very clear and I understood importance of pharmacology in practice. The learning sources provided are very useful.
Sir, before joining your classes I was very depressed because I could not clear POC II even after trying three times. Then I joined your classes for POC and came to know about my mistakes. In my fourth attempt I passed POC II because of your way of teaching.
