Wednesday, March 27, 2019

SAR sem 8

Synthesis

ANS-Cholinergic Drugs

ANS-Cholinergic Drugs

Cholinergic Drugs
Muscarinic agonists : methacholine, carbachol, bethanechol, pilocarpine
Acetylcholine esterase inhibitors : physostigmine, neostigmine*, pyridostigmine,
edrophonium, echothiophate, malathion, parathion, paraoxonC, sarin, pralidoxime
AntiAlzheimer’s : Tacrine*, donepezil, rivastigmine
Cholinergic antagonists : Atropine, scopolamine, homatropine, ipratropium
cyclopentolate*, dicyclomine*, benztropine, procyclidine, isopropamide, tropicamide
Ganglion blockers : (Self study- 1 hr) trimethaphan, mecamylamine, hexamethonium
Neuromuscular blockers :(Self study) tubocurarine, gallamine, succinylcholine,
decamethonium

Notes

cholinergics and anticholinesterases


Drug treatment of alzheimers disease

Neuromuscular blocking agents and ganglionic blockers-converted

ANS Drugs - Adrenergic Drugs

Adrenergic Drugs

Alpha adrenergic agonists: phenylephrine*, naphazoline, xylometazoline, oxymetazoline,
methyldopa, clonidine, guanabenz, guanafacine
Beta agonists : Isoproterenol, colterol, metaproterenol, terbutaline*, albuterol,
isoxsuprine, ritodrine
Alpha antagonist : tolazoline, phentolamine, phenoxybenzamine, prazosin, doxazosin
Beta Antagonists : pronethalol, propranolol*, pindolol, sotalol, timolol, atenolol,
metoprolol, esmolol, acebutolol, carvedilol, labetalol* (last two for self study, including
synthesis of labetalol)
Other adrenergic agents (Self study-2 hrs) : amphetamine, pseudoephedrine, ephedrine,
guanethidine, propylhexedrine, reserpine


Notes

Adrenergic Synthesis And Metabolism animation

Catecholamine Biosynthesis Pathway

mechanism of action of adrenergic receptor


Wednesday, February 20, 2019

Antidepressants Drugs

MAO Inhibitors (self study – 1 hr) Iproniazide, moclobemide, phenelzine, tranylcypromine;
imipramine*, chlorimipramine, amitriptyline, nortriptyline, doxepine*
fluoxetine*, paroxetine, sertraline, escitalopram, amoxapine

Monoamine oxidase as Drug Targets



Anticonvulsant Drugs

Types of seizures (Self study- 1 hr)
phenobarbital, mephobarbital, phenytoin, mephenytoin, ethotoin, trimethadione,
ethosuximide, methsuximide, phensuximide, diazepam, clonazepam, carbamazepine*,
valproic acid, vigabatrine, progabide, lamotrigine, tiagabine

Types of seizures

Animation Types of Seizures

Anticonvulsant Drugs I

Anticonvulsant Drugs II

Sedative Hypnotics


Sedative-hypnotics are drugs that depress or slow down the body's functions. Often these drugs are referred to as tranquilizers and sleeping pills or sometimes just as sedatives. Their effects range from calming down anxious people to promoting sleep.


Sedative Hypnotics

Sedatives – Hypnotics - Barbiturates 

Thyroid Hormones

Thyroid gland (weighs about 30 g in adults) is located on either side of the trachea below the larynx. It produces two principal hormones thyroxin (T4; 3,5,3',5'-tetraiodothyronine) and 3,5,3'-triiodothyronine (T3)-which regulate the metabolic rate of the body. Thyroid gland also secretes calcitonin, a Hormone Concerned with calcium homeostasis.

Classification:
Inhibit Hormone Synthesis (Anti thyroid Drugs):-
¢Propylthiouracil, Methimazole, Carbimazole
Inhibit Iodide Trapping (Ionic Inhibitors):-
¢Thiocynates (-SCN), Perchlorates (-ClO4), Nitrates(-NO3)
Inhibit Hormone Release:-
¢Iodine, Iodides of Na and K, Organic Iodide
Destroy Thyroid Tissue:-
¢Radioactive Iodine (131I, 125I, 123I)
 Thyroid hormone
    (Used to treat thyroid hormone deficiency)
   Levothyroxine, also known as L-thyroxine, is a manufactured form of the thyroid hormone, thyroxine (T4)


Thyroid Hormones

Thyroid Animation

Thyroid Hormone Synthesis and Antithyroid drugs

Calcium Homeostasis

Calcium Homeostasis

Calcium Homeostasis (Self study-1 hr)
raloxiphene, alendronate, teriparatide

Calcium Homeostasis

Vdo on calcium homeostasis

Monday, February 18, 2019

Anticonvulsant Drugs

Introduction
The term "anticonvulsant" is applied to a drug used for the treatment of epileptic seizures, hence, the synonym "antiepileptic.” Anticonvulsants are also being used in the treatment of neuropathic pain and as mood stabilizers in the treatment of psychiatric disorders such as bipolar disorder. In this article, the author reviews anticonvulsants as a drug class and their use in conditions other than epilepsy, such as pain and psychiatric disorders. The author also compares the mechanism of action as well as the efficacy of various anticonvulsants.
Key points
 
• A number of drugs with different mechanisms of action have anticonvulsant properties and are used as antiepileptics.
 
• Some of the approved anticonvulsant drugs have been investigated for relief of pain and psychiatric disorders and some of these indications are approved.
 
• Several clinical trials of anticonvulsant drugs are still ongoing.
 
• The use of anticonvulsants should be personalized to increase efficacy and safety by matching the right drug to the right patient.

Classification

Follow the link for Medicinal Chemstry & SAR presentation