Pharm Notes September 8

Absorption:
o Inhalation fastest route greater surface area
o Sublingual second fastest route
o Ionized forms are renally excreted charged structures
o Non ionized cross membranes
Bioavailability in first class effect goes down
Metabolism:
o Phase 1: oxidation reduction and hydroxylation
o Phase 2: sulfation and shit
Elimination
o Type 1: Phase 0:
o Type 2: Phase 1:
Partial agonist acts as a antagonist aginst full agonist
o Decreases the response of full agonist drugs
Non competitive drugs (indirect acting drugs) act on enzymes where as competitive drugs (direct acting drugs) act on receptors
o Non competitive = any curve that is not parallel
o Efficacy is the same between the two
Potentiation: increase in action of drug by addition of another drug
o Any curve that is parallel to the left side
Therapeutic index
o Importance of this test is to promote the safety of the drug
o LD50= lethal dose in 50% of the population
o ED50= efficient dose in 50% of the population
o Higher the therapeutic index the safer the drug is

AUTNOMIC NERVOUS SYSTEM

Parasympathetic: most commonly convers vegetative functions
o Motility and secretion of the GI tract
o Nicotinic receptors and muscarinic receptors
Nicotinic has two subtypes: nicotinic nerve and nicotinic muscle
Present at the ganglion
Muscarinic receptors has 3 subtypes: M1, M2,M3
Muscarinic are present at neuroeffector junction
o Most important ones are these
o AcH is the neurotransmitters that act on nicotinic and muscririnc receptors
Sympathetic: most commonly prepares the organs for emergencies flight or fight
o Nicotinuic receptors are found at the ganglion of sympathetic
o Alpha and beta receptors are seen at the nueroeffector junction
o Norepinephrine/ nor adrenaline acts on the neuroeffector junction
o AcH acts on nicotinic receptors only
Paraympathetic
Cholinergic drugs
o Cholinergic agonist drugs aka parasympathetic agonist drugs
o 1) Direct acting
Acts ONLY on receptors
Nicotine: AcH ester of choline
Muscarinic: bethanechol. ,methacholine, pilocarpine
o 2) Indirect acting
Reversible AchE inhibitors
Any drugs that end in STIGMINE are reversible
Physotigmine only one that crosses CNS IMPORTANCE

Endorophonium
Irreversible AchE inhibitors
Most commonly used by FARMERS
Pesticides and insecticides
o Echothiophate
o Malathion
o Parathion

AcH acts on:

o Eye (constriction contraction, excitation) , heart (inhibition, dilation, relaxation acts on SA and AV node ony) , lungs,
GIT, urinary bladder, glands
Ach has short half so therefore has no chemical use
Alzhemiers cerebral atrophy donepezil and tacta? Only two drugs you take progressive memory loss and dementia
situations only
OUT OF ALL CHOLINERGIC AGONST DRUGS ECOTHIPHATE IS THE BEST ONE AND IS USED FOR GLAUCOMA
o Pilocarpine is the second best choice
Bethanechol best for urinary bladder and bubble?

Sept 12. 2016

M2 is the only one that is present in the heart (SA and AV node) dilation
M2 receptors act as second messengers and act as inhibitory actions
GI secondary messengers decrease adenylate cyclase which decreases cAMP
o M1 acts on glands on GI tract contraction
o M1 and M3 are the same mechanism contractions
Increases intracellular calcium via increasing IP3

Nicotinic: has no second messengers

o Contraction of skeletal muscles
Only stigimine trhat crosses CNS is physiostigmine
Pyridostigimine used for the treatment of myasthenia gracvis
o Can pick any of cholingergic agoinst drugs

Cholinergic Antagonist Drugs

Act by blocking the drugs which act on nicotinic which blocks AcH
Drugs that block end receptors and enzyme drugs
M blocking drugs: cholinergic antagonist drugs
o Anti muscarinic drugs
Atropine, benztropine, scopolamine (motion sickness on boats), glycopyrolate, ipratropium, tropicamide, tribexyphenidyl
o Lungs- dilation so used for treatment of asthma
Sept 15 / 2016

Alpha 1 antagonist
o Doxazosin, prazosin, terazosin
Alpha 1 and beta agaonist carvedilol, iabetalol
o Mixed sympathetic drug
Beta blockers are important drugs for treamtnet of hypertension
o Because they have no effect on vasculature
Beta blockers
o Conditions:
2 beat blockers having ISA properties:
o acabutodol

o pindadol?
o