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Pharmacology > Lecture 10 (EXAM 2) > Flashcards

Lecture 10 (EXAM 2) Flashcards

1
Q

What are the cholinergic and adrenergic receptors?

A

Cholinergic: Parasympathetic -> Muscarinic, nicotinic, ganglionic

Adrenergic: Sympathetic -> alpha 1,2 / ß1,ß2, ß3

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2
Q

Why are nicotinic receptors, not the best drug targets?

A

Because there are widespread (ganglia, medulla, skeletal muscles, brain) and may cause multiple adverse effects

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3
Q

What are the sympathetic and parasympathetic effects on the eye (pupils)?

A

Sympathetic: contraction of the radial muscle
-> Pupils DILATED (bigger)

Parasympathetic: contraction of the Sphincter muscle
-> Pupils constricted (smaller)

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4
Q

Meaning of Mydriasis and Miosis

A

Mydriasis: Pupils dilated (bigger) - SYMPATHETIC

Miosis: Pupils constricted (smaller) - PARASYMPATHETIC

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5
Q

What are first and second messenger in signaling system?

A

-f.e. an agonist binding to the receptor would be the first messenger

-the G-protein associated with the receptor is the second messenger -> GDP cleaves off and GTP binds to the G-protein causing further downstream effects

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6
Q

What are the two metabolites that activate the signaling in the Phospholipase C pathway?

A

-DAG activating the protein kinase C (PKC)

-IP3 stimulating Ca release -> activating a protein kinase

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7
Q

How does the Acetylcholine pathway start?

A

-Cholin (with diet, f.e. bread) uptake by CHT (transporter)

-combined with Acetate to form Acetylcholine (with ChAT enzyme)

-ACh gets transported into vesicles

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8
Q

How is ACh released from the pre-synaptic nerve terminal?

A

Action potential comes down, and causes depolarization -> the voltage-dependent Ca-channel opens and Ca2+ activates vAMP

-vAMPs will cause the vesicle to fuse with the membrane -> which causes ACh release into the synaptic cleft

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9
Q

What is the role of Vesamicol?

A

It inhibits ACh uptake into the vesicles in the presynaptic neuron

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10
Q

What is the effect of the Botulinum toxin?

A

It inhibits vAMPS and prevents ACh release

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11
Q

How is the ACh activity stopped?

A

-Acetylcholine is broken down into Choline and Acetate by the Acetylcholineesterase

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12
Q

What are the effects of Parasympathomimetics?

A

-Things that act like ACh -> cholinergics

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13
Q

What are the muscarinic effects of the heart?

A
  • bradycardia (slow rate, negative chronotropy)
  • decreased conduction (negative dromotropy)
  • decrease contraction force (negative inotropy)

-some muscarinic effect of vasodilation

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14
Q

What are the Parasympathomimetic effects in the GI?

A

increased tone and motility of the wall muscles and relaxation of sphincters

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15
Q

What are the Parasympathomimetic effects on the bladder?

A

the body (detrusor mm) contracts while sphincters relax

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16
Q

Parasympathomimetic effects on the lungs

A

bronchoconstriction and increase secretion

17
Q

Parasympathomimetic effects on the eye

A

contraction of the ciliary mm (lens) and circular mm of the iris

18
Q

Parasympathomimetic effects on the exocrine glands

A

promotes secretion

19
Q

What is a Sludge response?

A

Response to an increased muscarinic stimulation
f.e. eating the wrong mushroom

20
Q

How are Cholinergic stimulants different from Acetylcholine?

A

-They have similar structures and are considered choline esters
-they have less vulnerable to Cholinesterase, different strengths of Muscarinic and nicotinic action

-Synonyms:
Parasympathomimetics
Cholinergic agonists
Muscarinic agonists
Cholinoceptor stimulants

21
Q

Examples of choline esters

A

-Methacholine (Acetylcholine with a methyl group)
-Carbachol (Amid group instead of an acetyl group)
-Bethanechol (Amid group and a methyl group)

22
Q

What is the indication of Bethanechol?
Cholinergic agonist

A

Brand name: Duvoid

postpartum and postoperative nonobstructive urinary retention and it also can counteract bladder dysfunction
-> relieve difficulties in urinating

23
Q

What is the indication of Carbachol?
Cholinergic agonist

A

Miotic agent (small pupils) -> Pupils contract

-treatment of glaucoma

24
Q

What are muscarinic agonists

A

-Natural alkaloids (not choline esters)

-Muscarine - considered a toxin -> from mushrooms, several types
no clinical use

-Pilocarpine – prototype (class representative)

25
Q

What is the indicational use of Pilocarpine?

A

-Natural alkaloid - prototype (the representative of a class to
which all others are compared)

-ophthalmic agent in tx of glaucoma, but other drugs are preferred

26
Q

How can Muscarinic toxicity be treated?

A

-With Atropine, a specific antidote
-it is a muscarinic antagonist, blocking muscarinic receptors

27
Q

What is the indication of Plecanatide (Truvance)?

A

-Muscarinic agonist
-binds on Guanylate Cyclase C (2nd messenger in intestinal epithelial cells + dopamine neurons in the brain)

-treats chronic idiopathic constipation by mimicking heat-stable enterotoxins (diarrhea)

Pharmacology (14 decks)

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