Pharmacology Cards

Question 1

Fat depot site

Answer 1

Lipophilic drugs accumulate here and are slowly released
eg. Thiopental and other aneasthetics(leads to increased sedation in obese patients)

Question 2

Bone depot site

Answer 2

Calcium binding drugs accumulate here
eg. Tetracycline in bone and teeth(leads to discolouration, yellow of teeth

Question 3

Liver depot site

Answer 3

Many drugs accumulate here due to affinity for hepatic cells
eg. Quinacrine(antimalarial) has higher concentration in liver than plasma

Question 4

Skin depot site

Answer 4

Eg. Griseofulvin binds to keratin in skin, hair and nails protecting them from infection
Chloroquine, highly tissue bound hence stays in body for a longer time

Question 5

Tyrosine hydroxylase inhibitor

Answer 5

Methyl tyrosine

Question 6

DOPA decarboxylase substrates

Answer 6

Methyl dopa-false substrate used in hypertension
Droxydopa-produces NE which can be used in orthostatic hypotension

Question 7

Enzyme converting NE to Epi

Answer 7

PNMT( increased levels in the adrenal gland as Epi is majorly produced in this gland). It’s level also increases in phaeochromocytoma and cortisol concentration

Question 8

Which of the enzyme in the catecholamine synthesis is dependent on copper

Answer 8

Dopamine ß- hydroxylase (hence its activity decreases in Wilson’s and Mendes disease)

Question 9

NET (uptake 1) inhibitor

Answer 9

Cocaine
SNRIs
TCAs

Question 10

Alpha adrenoceptors use which pathway in the receptor signalling

Answer 10

DAG and IP3(because it uses the Gq , Go, Gi)

Question 11

Beta adrenoceptors use which kind of pathway in the receptor signalling

Answer 11

cAMP(uses Gs to activate adenylyl cyclase to cause relaxation)

Question 12

ß1 receptor activation causes

Answer 12

Increase in inotropic, dromotropic and chrontropic effect in heart
Release of renin from the kidney

Question 13

Why are alpha 1 agonists used as nasal decongestants

Answer 13

Because the cause vasoconstriction leading to decrease in mucus secretions

Question 14

ß2 agonist are used in asthma treatment because

Answer 14

The can cause bronchodilation

Question 15

Examples of selective alpha1 agonist

Answer 15

Phenylephrine
Methoxamine
Midrodrine
Oxymethazoline
Xylomethazoline

Question 16

alpha2 selective agonists

Answer 16

Clonidine
Methyl dopa
Apraclonidine
Tizanidine
Guanfacine
Dexmedetomidine

Question 17

ß1 selective agonists

Answer 17

Dobutamine

Question 18

ß2 selective agonists

Answer 18

Albuterol(Salbutamol)
Terbutaline
Ritodine
And all the drugs with -terol

Question 19

ß3 agonist

Answer 19

Mirabegron

Question 20

Non-selective alpha inhibitors

Answer 20

Phenoxybenzamine
Phentolamine

Question 21

Alpha1 antagonists

Answer 21

Prazosin
Tamsulosin
Dozaxosin
All drugs ending with -zosin

Question 22

Alpha2 antagonist

Answer 22

Yohimbine
Rawuolscine
Tolazoline

Question 23

D1 selective agonist

Answer 23

Fenoldopam

Question 24

Dopamine activity is dependent on concentration. How?

Answer 24

Low conc. - Act on dopamine receptors to cause vasodilation in coronary, renal and mesenteric arteries
Intermediate conc. - Acts on ß receptors to cause increased chrontropic and inotropic effect
High conc. - Act on both alpha and beta receptors

Question 25

Non-selective ß receptors(1st generation)

Answer 25

Propanolol Timolol Pindolol Nadolol Penbutolol

Question 26

2nd generation ß1 antagonist

Answer 26

Bisoprolol Esmolol Metoprolol Are no lol Acebutolol

Question 27

3rd generation Non-selective ß antagonist

Answer 27

Carvedilol Labetalol

Question 28

3rd generation Selective ß antagonist(these are cardio selective and vasodilators)

Answer 28

Celprolol Nebivolol Butaxolol

Question 29

Butoxamine

Answer 29

Non-selective ß antagonist with more affinity for ß2

Question 30

In the treatment of both hypertension and BPH what drug alpha1 antagonist would be preferred

Answer 30

Prazosin cause it acts on both alpha 1b on vessel and alpha 1a on ureter

Question 31

Mixed antagonists

Answer 31

Ephedrine(alpha 1and2 & ß 1and 2) Epinephrine (alpha 1and2 & ß 1and 2) Norepinephrine (alpha 1and 2 & ß1)

Question 32

When there is an increase BP, the vasomotor centre is stimulated, increasing parasympathetic outflow. What does this cause?

Answer 32

Reflex Bradycardia

Question 33

In the case of decreased BP such that baroreceptor tone decreased leading to increase in HR and sympathetic vasoconstriction. What is this increase called?

Answer 33

Reflex tachycardia

Question 34

In ACh synthesis, choline is transported into the neuronal end using

Answer 34

Choline transporter

Question 35

Ziconotide

Answer 35

Inhibits calcium channel preventing infflux required for exocytosis

Question 36

Botulinum toxin

Answer 36

Inhibits actions of docking proteins SNAPS and VAMPS hence no exocytosis

Question 37

Alpha ketoacids and naptholquinones

Answer 37

Inhibits ChAT enzymes affect ACh synthesis

Question 38

Helicholinium

Answer 38

Inhibits choline transporter decreasing choline levels in neuronal end

Question 39

Vesamicol

Answer 39

Blocks VAT leading to release of empty vesicles

Question 40

Latrotoxin

Answer 40

Leads to an explosive release of ACh due to increased influx of calcium

Question 41

Physostigmine

Answer 41

Inhibits AChE increasing ACh levels in synapse

Question 42

Calcium

Answer 42

It's uptake causes exocytosis

Question 43

Atropine and tubocurarine

Answer 43

Inhibits acetylcholine receptors

Question 44

Types of ChEs

Answer 44

Aetylcholinesterases(true cholinesterase and breaksdown ACh only) in synapse and intact RBCs Butyrylcholinesterase(pseudocholinesterases) hydrolysis all other cholinesters except ACh. Widely spread in the body

Question 45

Muscarinic receptors are GPC receptors and work by,

Answer 45

Even numbered- work thro Gs pathway Odd numbered- work thro Gq pathway

Question 46

Factors helping with cholinester interaction with receptors

Answer 46

Bulkiness Structure [cationic head, alkyl group and ester/carbamate group]

Question 47

The modified ACh forms

Answer 47

Carbachol (modified ester group) Methacholine(modified alkyl group) Bethanecol/Urecholine(modified alkyl and ester group)

Question 48

Alkaloidal muscarinic agents

Answer 48

Muscarine(from Amanita Pilocarpine(

Question 49

How does high ACh concentration cause vasodilation

Answer 49

Increased ACh acts biphasically by Acting on its actual receptors And acting on Nn receptors on sympathetic nerves to cause the release of NE on alpha1 receptors

Question 50

In high dose of ACh, it acts on both M2 and Nn receptors. How are their effects seen

Answer 50

Due to high ACh levels, parasympathetic effects increase(seen first) but effects are short lived since AChE hydrolyzes it. Sympathetic effects are seen later but effects last longer since NE isn't easily brokendown

Question 51

Examples of Indirect acting agonist are Anti-Cholinesterases. What are the types.

Answer 51

Simple alcohols(short acting) - edrophonium(tensilon) Carbamates(intermediate acting) -Neostigmine, physostigmine, and the other -stigmines Organophosphates- sarin gas, soman gas , ecothiophate

Question 52

Types of anti muscarinic agents

Answer 52

Alkaloids- atropine, hyoscine, scopolamine Tertiary amines Quaternary amines

Question 53

Characteristics of tertiary amines and alkaloids cholinergic blockers

Answer 53

Lipid soluble Highly selective for muscarinic receptors Have CNS effects

Question 54

Ganglion stimulant examples

Answer 54

Alkaloids- nicotine (but not clinically used as the stimulate both PNS and SNS with both effects cancelling out) And others

Question 55

Other ganglion stimulants

Answer 55

Lobeline Epibatidine(from frog) Varenicline(used clinically in nicotine addiction) Tetramethyl ammonium Dimethyl phenylpiperazenium

Question 56

Examples of Ganglion blockers

Answer 56

Trimethaphan Pentolinium Hexamethonium Mecamylamine

Question 57

Types of Neuromuscular blockers

Answer 57

Depolarizing Non-depolarizing(acts as competitive antagonists hence gives flaccid paralysis. Actions can be reversed by increase in ACh levels)

Question 58

Examples of non-depolarizers

Answer 58

Gallamine(not in use) Vecuronium Pancuronium Rocuronium Atracurium Mivacurium

Question 59

Examples of depolarizers

Answer 59

Suxamethonium/Succinyl choline

Question 60

How depolarizers work

Answer 60

Phase 1- binds to receptors to cause continuous depolarization of the muscle Phase 2- desensitization of receptors

Question 61

Types of paralysis seen in non- depolarizing and depolarizing blockers

Answer 61

Depolarizing-Spastic paralysis(because paralysis follows contractions, they are more stiffer) Non-depolarizing- Flaccid paralysis

Question 62

How are effects of depolarizing effect reversed

Answer 62

By the use of suxamethonium since increase in alACh levels don't reverse it