Cholinergic And Adrenergic Drugs

Front 1

Nicotine

Back 1

Direct-acting cholinomimetic drug. Acts on Nicotinic Receptors.

Front 2

Muscarine

Back 2

Direct Acting cholinomimetic drug. Acts on muscarinic receptors.

Front 3

Nicotinic vs Muscarinic Receptors

Back 3

Nicotinic receptors are inotropic and form cation selective ion channels.

Muscarinic receptors are metabotropic and GPCRs. Often form dimers.

Front 4

What are indirect-acting drugs?

Back 4

They act to inhibit enzymes like Acetylcholine Esterase, which ultimately increases endogenous concentration of ACh available in synaptic clefts.

Front 5

What is Pilocarpine?

Back 5

Direct-acting cholinomimetic. Acts as a partial agonist of muscarinic receptors.

Front 6

Clozapine

Back 6

Inverse agonist of 5-HT receptors, can reverse constitutive activity. This is an "atypical antipsychotic."

(olanzapine).

Front 7

Typical Antipsychotics

Back 7

These are neutral antgonists.

Front 8

Receptor Desensitization Pathway

Back 8

Prolonged stimulation signals GRK (G-protein receptor kinase) to phosphorylate the receptor.

Arrestin binds, inactivates the receptor and targets for internalization.

Front 9

What are RAMPs?

Back 9

Receptor Activity Modifying Proteins that associate with GPCRs and can switch GPCR specificity from one ligand to another.

Front 10

Pharmacological Chaperones

Back 10

Membrane permeant non-peptide antagonists. These act intracellularly, and dramatically increase the expression of mutated GPCRs on the cell surface by allowing further time to fold and mature.

Front 11

Hemicholiniums

Back 11

Blocks the Choline-Na+ symporter.

Front 12

Vesamicol

Back 12

Blocks the Vesicle Associated Transporter (VAT) that transports ACh into vesicles.

Front 13

Botox (botulinum toxin)

Back 13

Degrades the SNAP25 protein on membranes and prevents fusion of vesicles containing ACh.

Front 14

Norepinephrine Synthesis

Back 14

(1) Tyrosine-->[Tyrosine hydroxylase]-->DOPA

(2) DOPA--> [DOPA Decarboxylase] --> Dopamine

(3) [Dopamine Beta-Hydroxylase] makes NE in vesicles.

Front 15

METYROSINE

Back 15

Inhibits tyrosine hydroxylase. Thus, inhibiting catecholamine synthesis.

Front 16

RESERPINE

Back 16

Inhibits VMAT, causes depletion of neurotransmitter stores.

Front 17

Cocaine and Tricyclic Antidepressants

Back 17

Inhibit NET, resulting in an increase of NE in the synaptic cleft.

Front 18

Tyramine, amphetamines, ephedrine

Back 18

All capable of releasing stored NT by Ca2+ independent process. The are avidly taken up by NET, and then transported by VMAT into vesicles, displacing NE-->reverse transported out of cell by NET.

Front 19

Heart receptors

Back 19

Heart has M2 muscarinic and B1, B2 adrenergic receptors.

Front 20

Carbachol

Back 20

Cholinomimetic that activates the ACh receptors.

Cholinergic Agonist-->used for treating glaucoma

Front 21

Methacholine

Back 21

Non-selective Muscarinic Receptor Agonist.

Front 22

Pilocarpine

Back 22

Partial agonist of the muscarinic receptor. Used for glaucoma and dry mouth. Eye drops--> stimulates M AChR causing mitosis and opening of canal of Schlemm.

Front 23

Neostigmine

Back 23

Indirect acting cholinomimetic.

Reversible.

Used for Mysthenia Gravis to increase ACh concentration to help with dec. receptors.

Post-op to stimulate pee pee.

Front 24

Edrophonium

Back 24

Reversible indirect acting cholinomimetic. Diagnostic tool for myasthenia gravis.

Alcohol with ammonium group.

Front 25

Isoflurophate

Back 25

Irreversible organophosphate that is an indirect acting cholinomimetic.

Front 26

Malathion

Back 26

Insecticiede.

An indirect acting cholinomimetic that is metabolized in humans but not insect.

Front 27

Sarin

Back 27

Nerve gas. Indirect acting cholinomimetic.

Treat with atropine and 2-PAM.

Front 28

Indirect Acting Cholinomimetics

Back 28

Inhibit cholinesterase and increase ACh. ACh stimulates both parasympathetic and sympathetic.

Vascular beds not affected b/c no endogenous ACh.

HR will fall b/c parasympathetic wins out (M2 receptors) over simp (B1, B2). ACh causes presynaptic inhibition of NE release.

Front 29

Atropine

Back 29

Muscarinic Receptor antagonist. Competitive. Blocks vagal tone.

Can cause long term mydriasis.

Front 30

Scopolamine

Back 30

Cholinoreceptor Antagonist.

suppresses emesis but also causes sedation and dry mouth.

Front 31

Benzatropine

Back 31

Cholinoreceptor Blocking.

Treats Parkinsonian Tremors.

Front 32

Ipratropium

Back 32

Block constriction, keeps airways open in asthma.