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Pharmacology > pharm exam 2 > Flashcards

pharm exam 2 Flashcards

1
Q

How is Acetylcholine made

A

made from using acetyl-CoA using enzyme Choline O-acetyltransferase

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2
Q

Where does the synthesis of ACh occur

A

in nerve fiber of the mitochondria

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3
Q

How does Ach make is to the neuronal terminal

A

by a choline transporter

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4
Q

How is the Ach stored?

A

as packages of quanta in vesicles on the surface of nerve terminal facing the synapse

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5
Q

how is Ach released?

A

an action potential is generated in the nerve. An influx of Ca+ interacts with the vesicle membrane triggering fusion to the terminal membrane. A pore then opens into the synapse and subsequent release of quanta into the synaptic cleft

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6
Q

What are the three ways thats adrenergic action can be terminated

A
  1. NE metabolized by catalytic enzymes (MAO)2. Diffusion away from receptor site (then metabolized)3. Re-uptake into terminal by norepinephrine transporter
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7
Q

What are receptors?

A

they are structures made out of protein that are designed to bind endogenous molecules

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8
Q

what are the two types of cholingergic receptors?

A

muscarinic and nicotinic receotors

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9
Q

what are the types of andrenergic receptors?

A

a1,a1, b1,b2 and dopamine

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10
Q

what part of the nervous system is often reffered to as trophotric

A

parasympathetic system

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11
Q

What is the function of the parasympathetic nervous system?

A

rest and digest, conserves and stores energy, stimulates digestive activity

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12
Q

What is the function of the sympathetic nervous system

A

fight or flight, means leading to energy expenditurestimulates heart, increase blood sugar, mediated vasoconstriction of blood vessels

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13
Q

what are the cardiovascular effects of parasympathetic nervous system

A

decrease heart rate

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14
Q

what are the cardiovascular effects of sympathetic nervous system

A

alters peripheral vascular resistance to manage BP, Heart rate, venous tone, renin production to manage renal blood flow

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15
Q

What is the function of the alpha 2 receptors.

A

present on noradrenergic nerve terminals.activated by binding of NE released from nerves.binding results in reduced release of more NE

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16
Q

what is an autoreceptor

A

is a receptor that responds to NE released from the same neuron that acts as an inhibitor

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17
Q

What is the function of Beta receptors

A

present on some neuronsFacilitate the release of more NE

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18
Q

what is a heteroreceptor

A

responds to neurotransmitters from other neurons

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19
Q

what are the 2 mechanisms for postsynaptic regulation

A

up or down regulate receptorsaction of one receptor is affected by the action of another

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20
Q

what are the two key actions of Ach at the muscarinic receptors in the parasympathetic NS

A
  1. nerves in parasympathetic NS release ACh that activates muscarinic receptors on target organs. This alters organ function by creating a positive stimulus2. ACh is released from nerves of parasympathetic NS bind to receptors on nerve terminals to inhibit release of other neurotransmitters creates a negative stimulus
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21
Q

What is the role of nicotinic receptors in autonomic NS

A

located at ganglionic level of both parasympathetic and sympatheticBoth bind ACh released from pre-ganglionic neurons and pass message on to pos-ganglionic neurons.No ability inhibitory capabilities

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22
Q

What is the role of ACh at Nicotinic receptors in the Somatic NS

A

Found at the neuromuscular junction of skeletal muscle.Binding of ACh or an agonist causes depolarization of nerve cell causing contraction.prolonged binding to the receptor causes postganglionic neuron to stop firing prevent further depolarization causing muscle paralysis

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23
Q

what is a cholinomimetic

A

it is a nonacetylcholine compound that mimics the action of ACh

24
Q

What are the 2 ways that a cholinomimetic agent acts

A

They can act as direct agonist and bind to ACh receptors.They can act as indirect agonist.By inhibiting ACh hydrolysis preventing its break down

25
Q

Muscarine and nicotine are examples of what types of compounds

A

cholingergic compoundsThey are alkaloids derived from plants.They produce actions that mimic those seen when ACh binds to muscarinic receptors of the parasympathetic nervous system

26
Q

What are the 5 types of muscarinic receptors

A

M1-M5M1,M3,M5 cause cellular excitationM2,M4 inhibit cellular excitability

27
Q

Where are muscarinic receptors mainly found

A

on autonomic effector organsheart, smooth muscle, brain, exocrine glands

28
Q

What are the two types of nicotinic receptors

A

Nm which are located at the neuromuscular junctionNn which are located anywhere elseCNS,Adrenal medulla, autonomic ganglia

29
Q

what are the 2 groups of direct acting cholinomimetics

A

esters of choline and alkaloids

30
Q

what are choline esters

A

quarternary ammoniums that are insoluble in lipids but water soluble

31
Q

What are the characteristics of quarternary ammoniums

A

hydrophilic- poorly penetrate CNSHydrolyzed by AChEVariations in chemical structure alter characteristics

32
Q

what type of amine are cholinomimetic alkaloids

A

tertiary aminesexamples:pilocarpinenicotinelobeline

33
Q

what are characteristics of cholinomimetic alkaloids

A

well absorbed after oral administrationlipid solubility allows for a larger volume of distribution not susceptible to AChE

34
Q

how do indirect cholinomimetics act

A

they inhibit AChE

35
Q

what are the 3 types of AChE inhibitors

A

Simple alcohols with quarternary ammonium- edrophoniumCarbamate esters of alcohols with quarternanry or tertiary ammoniumorganophosphates

36
Q

what is the order of binding between AChE inhibitors for simple alcohols, carbamates esters, and organophosphates

A

simple alchohols> carbamate esters> organophosphates

37
Q

what are the effects of cholinomimetics on the eye

A

the eye is sensitive to muscarinic agonists and AChE inhibitorsThe end result causes contraction of the iris sphincter smooth muscle resulting in miosis.these facilitate flow of aqueous humor out of anterior chamber and alter amount and focus of light reaching retina

38
Q

what are some clinical uses of cholinomimetics

A

glaucoma muscarinic agonists and AChE inhibitors reduce intra-ocular pressure in narrow and wide angle glaucoma.Drugs: pilocarpine and physostigmine

39
Q

what are the effects of cholinomimetics on respiratory system

A

cause contaction of smooth muscle in bronchial tree (restricts air flow)also stimulates secretions from tracheobroncial mucosa

40
Q

What are the effects of cholinomimetics on the GI tract

A

increase secretory and motor activity in the gut.stimulates salivary and gastric glands, pancreas and small intestine,increases peristalsisrelaxes most GI sphincters allowing GI contents to pass along tract

41
Q

What are the effects of cholinomimetics on the GU tract

A

triggers voiding of bladder.stimulates detrusor muscle and relax the trigone and sphincter muscles of bladder

42
Q

what are the clinical applications of Cholinomimetics in GU disorders

A

corrects depressed smooth muscle activitytreats urinary retention

43
Q

what are the effects of direct cholinomimetics on the CV system

A

reduce peripheral vascular resistancedecreases heart ratenot used much because there are better medicines out there

44
Q

what are the effects of indirect cholinomimetics on the CV system

A

cause negative chronotropic- bradycardiacauses negative inotropic- drop in cardiac outputcauses modest drop in blood pressure

45
Q

what are the effects of direct cholinomimetics on the CNS

A

nicotinic receptors have been found to:induce tremorsstimulate emesisstimulate respiratory centermuscarinic receptors have been found to:induce tremorcause hypothermiainterfere with nociception

46
Q

what are the effects of indirect cholinomimetics on the CNS

A

low conc. little effecthigh concentrations cause convulsions, coma, respiratory arrest

47
Q

what are some uses of cholinomimetics for CNS conditions

A

Alzheimer’s disease-result from deficiency of cholinergic neurons in CNSSmoking cessation- decreases cravings and pleasurable effects of cigarettes

48
Q

how does ACh exert its affect at the neuromuscular junction

A

ACh is released from presynaptic neurons, ACh binds to nicotinic cholinergic receptors on the muscle fiber, this results in depolarization of muscle fiber that leads to skeletal muscle contraction

49
Q

what happens at the neuromuscular junction when low doses of AChe are used

A

they prolong the effects of ACh and increase the strength of muscle contraction

50
Q

what happens at the neuromuscular junction when medium doses of AChe are used

A

may cause muscle to fibrillate making the muscles less effective

51
Q

what happens at the neuromuscular junction when high doses of AChe are used

A

blocks muscle depolarization which leads to paralysis

52
Q

at what does is nicotine toxic

A

fatal at doese >40mg (1 drop of pure nicotine liquid)2 cigarettes contain about 40mg, but most of it is burned off in smokeif ingested by infants can cause vomiting

53
Q

what are some symptoms of someone who has muscarinic excess

A

miosis, salivation, sweating, bronchial constriction, diaphragm paralysis, vomiting, diarrhea

54
Q

how do you treat someone who is exposed to pesticides or organophosphates

A

monitor VS, decontaminate if possible, antidote with parenteral atropine or pralidoxime (2-pam)

55
Q

how does 2-pam work in a person who has pesticide exposure

A

2-pam reactivates inhibited AChE before the full covalent bond form through aging

Pharmacology (14 decks)

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