🔴 DEFINITION

🔸pA2
-pA2 is ameasure of the potency of an antagonist. It is the negative logarithm of the molar concentration of an antagonist that would produce a 2-fold shift in the concentration response curve for an agonist.

🔸IC50
-IC50 defines the molar concentration of an agonist or antagonist which produces 50% of its maximum possible inhibition in a functional assay. In a radioligand binding assay, IC50 defines the molar concentration of competing ligand which reduces the specific binding of a radioligand by 50%.

🔸EC50
-EC50 defines the molar concentration of an agonist that produces 50% of the maximum possible response for that agonist.

🔸pD2
-pD2 is the negative logarithm of an EC50 or IC50 value.

🔸pIC50
-pIC50 is the negative logarithm of the IC50 value.

🔸potency
-Potency is a measure of the concentration of a drug at which it is effective.

🔴DEFINITION

🔶Autonomic nervous system=

A part of the nervous system that regulates key involuntary functions of the body, including the activity of the heart muscle; the smooth muscles, including the muscles of the intestinal tract; and the glands.

🔶Sympathetic nervous system=

A part of the nervous system that serves to accelerate the heart rate, constrict blood vessels, and raise blood pressure.

🔶Parasympathetic nervous system =

The part of the involuntary nervous system that serves to slow the heart rate, increase intestinal and glandular activity, and relax the sphincter muscles.

🔶 Teratogenicity=

It refers to the capacity of the drug to cause foetal abnormalities when administered to the pregnant mother.

🔶Gout =

It is the metabolic disorder characterized by hyperuricaemia i.e. uric acid deposited in the joints.

🔴Mechanism of drug absorption

The three broad categories of drugs transport mechanism involved in absorption are:--

📌Transcellular/ intercellular transport
📌Paracellular /intracellular transport
📌 Vesicular or Corpuscular transport

🔹 Transcellularlar/ Intracellular Transport :- It is defined as passage of drug across the GI epithelium. it is most common pathway for drug transport .The 3 steps involved in trancecellular transport of drugs are__
(1)Permeation of GI epithelial cell membrane, a lipoidal barrier this is the major obstacle to drug absorption.
(2) Movement across the intercellular space (cytosol).
(3) Permeation of the lateral of basolateral membrane --
This is of secondary importance.
The virus transcellular transport process involved in drug absorption are :--

🔸Passive transport process :
This transport process do not require energy or other than that of molecular motion (Brownian motion) pass through the lipid bilayer. passive transport process can be further classified into following type.--
(a) Passive diffusion.
(b) Pore transport
(C) ion pair transport.
(d) facilitated or Mediated diffusion
🔸 Active transport process :-
These transport process require energy from ATP to move drug molecule from extracellular to intracellular milieu.They are of two types --
(a) Primary active transport
(b) secondary active transport--- this process is further subdivided into two--
(1) symport (co-transport)
(2) Antiport (Counter-transport)

🔹Paracellular/Intracellular Transporte :-
It is defined as the transport of the drugs through the junction between the GI epithelial cells. This pathway is of minor importance in drug absorption.The two paracellular transport mechanism involved in the absorption are--
🔸Permeation truth tight junction of epithelial cells:-
This process basically occurs through opening which are little bigger than the aqueous pores. Compounds such as insulin and cardiac glycosides are taken up by the mechanism
🔸Persorption :-
It is Persorption address through temporary opening fromed by shedding of two negighbouring cells into the lumen.

◾Paracellular transport differ from pore transport in that involves transfer of drugs across with epithelium and through the cellular junctions whereas in the case of latter,the molecules are transferred from outside of epithelium cell into the space through pores present in the cells in membrane.

🔹Vesicular or Corpuscular transport (Endocytosis) :-Active transport these are also energy depended process but involved transport, of within vesicles into a cell since the mechanism involves transport across the cell membrane, the process can also be classified as transcellular services Sula transport of drug can be classed into two categories__
🔸Pinocytosis(Cell eating) :- Adsorptive uptake of solid particulates.
🔸Phagocytosis(Cell drinking) :- Uptake of fluid solute.

🔴MECHANIAM OF ACTION

📌ACETYLCHOLINE
It is the chief neurotransmitter of the parasympathetic nervous system, the part of the autonomic nervous system (a branch of the peripheral nervous system) that contracts smooth muscles, dilates blood vessels, increases bodily secretions, and slows heart rate.

📌PILOCARPINE
▪Pilocarpine is a drug that acts as a muscarinic receptor agonist.
▪It acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract - resulting in pupil constriction (miosis). ▪Pilocarpine also acts on the ciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens the trabecular meshwork through increased tension on the scleral spur.
▪This action facilitates the rate that aqueous humor leaves the eye to decrease intraocular pressure. ▪Paradoxically, when pilocarpine induces this ciliary muscle contraction (known as an accommodative spasm) it causes the eye's lens to thicken and move forward within the eye. This movement causes the iris (which is located immediately in front of the lens) to also move forward, narrowing the Anterior chamber angle. ▪Narrowing of the anterior chamber angle increases the risk of increased intraocular pressure.

🔴Drug Effects Of Cholinergic Drugs🔴

📌 "MSLUBDD"📌

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➡️Miosis
➡️Salivation
➡️Lacrimation
➡️Urination
➡️Bronchoconstriction
➡️Defaecation
➡️Decreased Heart Rate