Drugs Modulating ANS Function (Cholinergic and AntiCholinergic Drugs)

Question 1

What are the two Cholinergic Receptors

Answer 1

Nicotinic, Muscarinic

Question 2

What drug are all muscarinic sites blocked by

Answer 2

Atropine

Question 3

What drug blocks Effector cells of skeletal muscle innervated by somatic nerves

Answer 3

Curare

Question 4

What drug blocks Autonomic ganglion cells of sympathetic & parasympathetic nerves

Answer 4

hexamethonium

Question 5

What drug blocks Adrenal medullary cells and some adrenergic nerve terminals

Answer 5

hexamethonium

Question 6

What are the locations of M1 receptors

Answer 6

CNS
Gastric Gland
Salivary Gland

Question 7

What are the locations of M2 receptors

Answer 7

Heart
GIT
CNS

Question 8

What are the locations of M3

Answer 8

Salivary Gland
Gastric Gland
Eye
GIT
Blood vessels

Question 9

What drug inhibit Cholinesterase

Answer 9

Neostigmine

Question 10

What drug inhibit AcH release by inhibiting synthesis

Answer 10

Hemicholinium- blocks choline uptake

Botulinium, Mg, aminoglycosides- inhibit release mechanism

Question 11

What drug blocks the action of AcH

Answer 11

Atropine, Tubocurarine

Question 12

What are the two types of Cholinergic Agonists

Answer 12

Direct Acting Agonist

Indirect Acting

Question 13

What type of Cholinergic Agonist inhibit acetylcholinesterase

Answer 13

Indirect Acting

Question 14

What substance may cause respiratory paralysis after large doses due to inhibition of presynaptic release of Ach & post-synaptic sensitization to Ach

Answer 14

Aminoglycosides

Question 15

What are the two types of Cholinoreceptor activating drug

Answer 15

Choline ester, Alkaloids

Question 16

What are the Choline Esters drugs

Answer 16

Acetylcholine
Metacholine
Bethanechol

Question 17

What are the Alkaloid drugs

Answer 17

Pilocarpine
Muscarine
Nicotine
Labeline

Question 18

What are the different types of cholinesterase inhibiting drugs

Answer 18

Alcohol
Carbamates
Organophosphates

Question 19

What are some examples of Organophosphates

Answer 19

Therapeutics
Insecticides
Nerve Gases

Question 20

True or false, the effects of AcH is short lived

Answer 20

True

Question 21

What are the main receptors that acetylcholine act on

Answer 21

Muscarinic and nicotinic

Question 22

Why are nicotinic effects not normally seen

Answer 22

Ach does not readily penetrate tissues which surround skeletal m & autonomic ganglia

Question 23

What are adverse effects of AcH

Answer 23

Diarrhoea and decreased blood pressure
Urination
Miosis
Bronchoconstriction & bradycardia
Excitation of skeletal m
Lacrimation
Salivation & sweating

Question 24

Nicotinic Effects of Acetylcholine can be protected based stimulation of nicotinic receptors on

Answer 24

Sympathetic and Parasympathetic Ganglia
Adrenal Medulla
Skeletal M

Question 25

What is the therapeutic use of Acetylcholine

Answer 25

Miosis during ophthalmic sx | (rarely use b/c of widespread effects & rapid hydrolysis by cholinesterase

Question 26

What are the adverse effects of Acetylcholine

Answer 26

Generalized cholinergic stimulation

Question 27

What receptors does Acetylcholine activate

Answer 27

M, N

Question 28

What is the therapeutic use of Bethanechol

Answer 28

Increases intestinal motility esp after sx. Stimulates detrusor m of bladder →used to treat urinary retention

Question 29

What are the adverse effects of Bethanechol

Answer 29

Generalized Cholinergic Stimulation

Question 30

What receptors does Bethanechol activate

Answer 30

M and some mild N properties

Question 31

What is the therapeutic use of Methacholine

Answer 31

Diagnosis of asthma and bronchial hyperactivity

Question 32

What are some adverse effects of Methacholine

Answer 32

Generalized cholinergic stimulation

Question 33

What receptors does Methacholine activate

Answer 33

M

Question 34

What is the therapeutic use of Pilocarpine

Answer 34

Very good at stimulating miosis & opening of trabecular meshwork around canal of Sclemn► used treatment of glaucoma

Question 35

What are the adverse effects of Pilocarpine

Answer 35

Unlike other direct acting agonists, pilocarpine is able to enter brain & cause CNS disturbances -hallucinations, convulsions & generalized cholinergic stimulation

Question 36

What receptors does Pilocarpine activate

Answer 36

M

Question 37

Give an example of Cholinesterase inhibiting drug Alcohols

Answer 37

Edrophonium

Question 38

Give an example of Cholinesterase inhibiting drug Carbamates : Teritiary Animes

Answer 38

Physostigmine

Question 39

Give an example of Cholinesterase inhibiting drug Carbamates: Quaternary Ammoniums

Answer 39

Neostigmine | Pyridostigmine

Question 40

Give an example of Cholinesterase inhibiting drug : Organophosphate: Therapeutics

Answer 40

Isoflurophate Echothiophate

Question 41

Give an example of Cholinesterase inhibiting drug : Organophosphate Insecticides

Answer 41

Malathion | Parathion

Question 42

Give an example of Cholinesterase inhibiting drug : Organophosphate Nerve Gases

Answer 42

Sarin

Question 43

What is the therapeutic use of Physostigmine

Answer 43

For overdoses of atropine, phenothiazines, tricyclic antidepressants

Question 44

What are the adverse effects of Physostigmine

Answer 44

Convulsions Muscle paralysis secondary to overstimulation Generalized cholinergic stimulation

Question 45

What is the therapeutic use of Neostigmine

Answer 45

Treatment of myasthenia gravis Treatment of urinary retention & paralytic ileus Antidote for non-depolarizing neuromuscular blockade as with tubocurarine

Question 46

What are the adverse effects of Neostigmine

Answer 46

Excessive cholinergic stimulation

Question 47

True or false, Neostigmine actions are more prominent on CVS and eye than NMJ and GIT

Answer 47

False, more prominent on NMJ and GIT than CVS and eye

Question 48

What is the therapeutic use of Endrophonium

Answer 48

Used to diagnose myasthenia gravis (MG). Not useful for maintenance therapy – short duration of action ( 5-15 min) Used to differentiate MG from cholinergic crisis (excessive Ach)

Question 49

True or False, In the test for Myasthenia Gravis, Edrophonium will drastically improve in patients with chollinergic weakness than Myasthenia Gravis

Answer 49

False, myasthenic weakness substantially improved by edrophonium; cholinergic weakness is aggravated

Question 50

What is the therapeutic use of Pyridostigmine

Answer 50

Long duration of action | Used for long term treatment of myasthenia gravis

Question 51

What is the adverse effects of Pyridostigmine

Answer 51

Excessive Cholinergic Stimulation

Question 52

What organophosphate is not highly lipid soluble

Answer 52

Echothiophosphate

Question 53

Recovery of enzymatic Activity in organophosphate depends on

Answer 53

Synthesis of new enzymes- process that may take weeks

Question 54

What is used to treat organophosphate Toxicity

Answer 54

Support respiration Very high doses of atropine (muscarinic receptor) Cholinesterase reactivator- Pralidoxime

Question 55

What are the different types of Neuromuscular blocks

Answer 55

Neuromuscular Ganglionic Muscarinic

Question 56

What are the drugs associated with muscarinic blockers

Answer 56

``` Atropine Scopolamine Homatropine Cyclopentolate Tropicamide Pirenzepine ```

Question 57

What are the types of Neuromuscular blockers

Answer 57

Non-depolarizing | Depolarizing

Question 58

What are the drugs associated with ganglionic blockers

Answer 58

Nicotine Hexamethonium Trimethaphan

Question 59

What are the therapeutic uses of atropine

Answer 59

Treatment of bradycardia Mydriasis & Cycloplegia Gastrointestinal spasms Organophosphate poisoning

Question 60

What are the toxic affects of Atropine

Answer 60

Red as a beet , blind as a bat , dry as a bone , hot as a hare & mad as a hatter “ → Cutaneous vasodilation → atropine flush , blurred vision , ↓ secretions , hyperthermia ( atropine fever due to ↓ sweat ), delirium & hallucinations

Question 61

What drug classes may have Anticholinergic side effects

Answer 61

``` Antihistamines Antipsychotics Tricyclic antidepressants Monoamine oxidase inhibitors ( MAOI ) Lithium ```