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S3M1-ANS Pharm
Ross University
57
Pharmacology
Professional
05/28/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
What is the typical location for Nicotinic neuronal receptor (Nn)?
Definition
ganglionic neurons** (fast EPSP)
adrenal medulla, some presynaptic cholinergic terminals, CNS neurons
Term
Waht is the typical location for Nicotinic muscular receptors (Nm)?
Definition
skeletal neuromuscular endplates
Term
What is the typical location for the M1 receptor?
Definition
Ganglionic neurons** (early slow EPSP)
some presynaptic terminals, CNS neurons
Term
What is the typical location for M2 receptors?
Definition
Myocardium** (THINK 2 of HEARTs),
presynaptic terminals**
ganglionic neurons (IPSP),
some smooth muscle,
CNS neurons
Term
What is the typical location for M3 receptors?
Definition
Smooth muscle**, exocrine glands**, vascular endothelium**, CNS neurons
Term
What is the main postreceptor mechanism of M1 receptor type?
Definition
Gq protein, where there is an increase in phospholipase C which causes an increase in IP3/DAG system and there is a closing of K+ channels
(note M3 has similar mechanism)
Term
What is the main post receptor mechanism for M2 receptor type?
Definition
Gi protein causes a decrease in cAMP and/or opening of K+ channels
Term
What is the main post receptor mechanism for M3 receptor type?
Definition
Gq protein, an increase in phospholipase C causing an increase in IP3/DAG system.
Term
Monoamine oxidase (MAO)
Where is it localized?
substrate specificity?
Isozymes?
Definition
localized: in mitochondrial membrane of hepatic, kidney, and nueronal cells
Has a low substrate specificity.
Isozymes: Has two isozymes
MAO-A: oxidates indolamines
MAO-B: oxidates catecholamines (i.e. takes part in catecholamine metabolism after they are released into the synaptic cleft i.e. metabolizes NE, however this is not hte primary mechanism of postjunctional activity, the primary mechanism is reuptake into the cell)
Term
Catechol-O-methyl-transferase (COMT)
Where is it localized?
What is the process of metabolism of epinephrine and norepinephrine?
metabolism of Dopamine by COMT?
Definition
Localized: in cytoplasm of most cells but is scarce in adrenergic neurons.
metabolism of epi and norepi: when located intraneuronally, they are deaminated by MAO and then methylated by COMT, but: when extraneuronally located they are methylated by COMT and then deaminated by MAO yielding in both cases= vanillymandelic acid

Dopamine metabolism: similar to epi and norepi with MAO and COMT yielding final metabolite of= homovanillic acid
Term
What is the typical location of Alpha 1 receptors?
Definition
Vascular smooth muscle**(has primarily alpha 1 receptors)
visceral smooth muscle(mainly sphincters)
radial msucle of iris
CNS neurons
Term
What are the typical locations of Alpha-2 receptors?
Definition
Some presynaptic terminals**
pancreatic islets (beta cells)
platelettes
ciliary epithelium
smooth muscle
CNS neurons
Term
What are the primary locations of beta-1 receptors?
Definition
myocardium**
JG cells**
some presynaptic terminals
adipocytes
CNS neurons
Term
What are the typical locations of Beta-2 receptors?
Definition
visceral smooth muscle**
vascular smooth muscle**
liver**
myocardium
skeletal muscle
some presynaptic terminals
CNS neurons
Term
What is the typical location of Beta-3 receptors?
Definition
adipocytes
Term
What is the typical location for D-1 receptors?
Definition
Vascular smooth muscle (renal and mesenteric vascular beds)**
CNS neurons
Term
What is the typical location for D-2 receptors?
Definition
Some presynaptic terminals,
CNS neurons
Term
Which adrenergic receptors are coupeled to Gs protein and cause an increase in cAMP?
Definition
Beta1 (also opens voltage gated CA++ channels (L type))
Beta2
Beta3
D1
Term
What are the major (2) post receptor mechanisms for the Alpha-1 receptor which is coupled to Gqprotein?
Definition
1. increase in phospholipase C causing an increase in IP3/DAG (same as M1 and M3 receptors)

2. increase in phospholipase A2 causing an increase in eicosanoid synthesis
Term
Describe the postreceptor mechanisms for Alpha 2 receptor coupled to Gi and G0 protein?
Definition
Gi: decrease in cAMP
Gi: opening of ligand gated K+ channels
G0: bloackade of voltage gated Ca2+ channels (Land N type)
Term
Describe the postrceptor mechanisms for D-2 receptors coupled to Gi and Go proteins
Definition
Gi: opening of ligand gated K+ channels
Go: blockade of voltage gated Ca2+ channels
Term
when does ACH have an inhibitory response?
What receptor does it act on?
What is the mechanism?
Definition
When ACH activates M2 receptors
This stimulates the release of dopamine or norepinephrine from small intensely fluorescent cells (SIF)
Which causes the opening of ligand-gated K+ channels
This leads to IPSP
Term
what 6 receptors are involved in ganglionic neurotransmission?
What neurotransmitter is involved?
what is their AP type?
Definition
1. Nn-ACH-fast EPSP
2. M1-ACH-early slow EPSP (several seconds)
3. Peptidergic-peptides-late slow EPSP (lasting several minutes)
4. M2-ACH-IPSP
5.D2-Dopamine-IPSP
6. Alpha-2-NE-IPSP
Term
In the periphery, most PNS target organs will have which receptor type?
Definition
M3
Term
cholinergic/PNS for the eye: give the response and recpetor for each: 1. sphincter of iris 2. ciliary muscle 3. lacrimal glands
Definition
1. sphincter of iris contracts-M3 2. Ciliary muscle: contraction -M3 3. Lacrimal glands-secretion-M3
Term

adrenergic/SNS effect on the eye: give the response and receptor

1. radial muscle of the iris

2. ciliary muscle

3. superior tarsal muscle

4. ciliary epithelium

Definition
1. radial muscle of iris: contraction/dilation of pupil- alpha1 2. ciliary muscle -relaxation-Beta 2 3. superior tarsal muscle - contraction-alpha1 4. ciliary epithelium: -increase aqueous humor production-beta2 -decrease aqueous humor production-alpha2 2.
Term

cholinergic/PNS effects on the lung:response and receptor

1. bronchial muscle

2. secretions

Definition

1.bronchial muscle: contraction: M3

2.secretions: increase:M3

Term

adrenergic/SNS on the lung: effect and receptors?

1. bronchial muscle

2. secretions

Definition

1. bronchial muscle-relaxation- Beta2

2. secretions-decrease - alpha1

increase secretions-beta 2

Term
anhydrosis
Definition
no sympathetic outflow so no sweating
Term
the neurotransmitter of the postganglionic sympathetic nerve for sweating is what?
Definition
ACH and not norepi
Term

In skin,(adrenergic/SNS) what type of effect and which receptor type are used for 1. pilomotor muscles (goosebumbs)

2. apocrine sweat glands

Definition

1. pilomotor muscles-contraction-alpha 1 receptors

2. apocrine sweat glands-secretion- alpha 1 receptors

Term
cholinergic/PNS effects on skin sweat gland ? receptor type?
Definition
secretion -M3 receptors
Term

Effects of cholinergic/PNS on GI tract and receptors:

1. motility and tone

2. lower esophageal sphincter

3. other sphincters

4. glands (salivary, gastric, etc..)

Definition
1. motility and tone will increase -M3 2.Lower esophageal sphincter-contract-M3 3. other sphincters-relaxation-indirect effect 4. glands-watery secretion-M3
Term
Effects on cholinergic/PNS gallbaladder and ducts, receptor? Effects of adrenergic/SNS on gall bladder, ducts and receptor?
Definition

cholinergic/PNS: contraction-M3

adrenergic/SNS: relaxation Beta 2

Term

adrenergic/SNS effects on the GI and receptors:

1. glands

2. motility and tone

3. spchincters

Definition

1. thick secretion Beta receptors

2. motility and tone - relaxed- alpha1, alpha2, beta2

3. sphincters-contraction-alpha 1

Term

cholinergic/PNS effects on the pacreas and receptors?

1. exocrine secretion

2. insulin secretion

Definition

1. exocrine secretion-increases M3

2. insuline secretion-increases M receptors

Term

adrenergic/SNS effects on pancreas and receptors?

1. exocrine secretion

2. insulin secretion

3.glucagon secretion

Definition

1. exocrine secretion decrease-alpha

2. insulin secretion decrease- alpha 2 (increase insulin with beta2)

3. glucagon secretion increase Beta

Term
adrenergic/SNS effect on liver and receptors?
Definition

increase glycogenolysis (B2>>A1) increase gluconeogensis (B2>>A1)

 

PNS doesnt have any significant effect on the liver

Term

cholinergic/PNS effects on sex organs and receptors

1. corpora cavernosa

2. uterus

Definition

1. corpora cavernosa-erection-M3 via NO

2. uterus- variable effect- M3

Term

cholinergic/SNS effect on sex organs and receptors?

1. vas deferens, seminal vesicle prostate

2. non pregnant uterus

3. pregnant uterus

Definition
1. ejaculation - alpha1 2. non pregnant uterus- relaxation -beta 2 3. pregnant uterus- relaxation beta2 contraction-alpha1
Term

cholinergic/PNS effect on urinary bladder and receptors?

1. detrusor (motility and tone)

2. trigone and sphincter

Definition
1. detrusor -increase motility and tone-M3 2. trigone and sphincter relaxation-indirect effects
Term
adrenergic/SNS on kidney and receptors?
Definition
increases renin secretion -beta 1 (remember beta 1 are only in heart and JG cells of kidney)
Term
What is the dominant ans system for blood vessels?
Definition
sympathetic
Term
cholinergic/PNS on arerioles and receptor?
Definition
dilation - M3 via NO (pns has negligible effects on veins)
Term
adrenergic/SNS effects on arterioles and receptors? 1. various organs 2. coronary, pulmonary 3. skeletal muscle 4. liver
Definition
1. various organs-constriction-alpha 1 2. coronary, pumonary -dilation-indirect effects 3. skeletal muscle-dilation-beta 2 4. liver- dilation -beta 2
Term
adrenergic/SNS effects on veins and their receptors?
Definition
constriction- alpha1 dilation-beta 2 remember that PNS has negligible effects on veins, so it is predominantly controlled by SNS
Term
adrenergic/SNS effect on spleen capsule and receptor?
Definition
spleen capsule contraction by Alpha1
Term

adrenergic/SNS on the heart and the accompanying receptors?


1. Heart: SA node rhythm

2. Atrium

a. conduction

b. refractoriness

c. automaticty

d. contractility

3. AV node

a. conduction

b. refractoriness

c. automaticity

4. ventricle

a. conduction

b. refractoriness

c. automaticity

d. contractility

Definition

remember: for all responses of SNS B1 is better than B2 (B1>>B2)

 

 

1. Heart: SA node rhythm increases : B1

2. Atrium

a. conduction: increases B1

b. refractoriness: decreases B1

c. automaticty increases B1

d. contractility increases B1

3. AV node increases B1

a. conduction increases B1

b. refractoriness decreases B1

c. automaticity increases B1

4. ventricle increases B1

a. conduction increases B1

b. refractoriness decreases B1

c. automaticity increases B1

d. contractility increases B1

 

Term

cholinergic/PNS on the heart and the accompanying receptors?


1. Heart: SA node rhythm

2. Atrium

a. conduction

b. refractoriness

c. automaticty

d. contractility

3. AV node

a. conduction

b. refractoriness

c. automaticity

4. ventricle

a. conduction

b. refractoriness

c. automaticity

d. contractility

 

Definition

 

1. Heart: SA node rhythm decreases: M2

 

2. Atrium

a. conduction increase M2

b. refractoriness decrease M2

c. automaticty decrease then increase M2

d. contractility decrease M2

 

3. AV node

a. conduction decrease M2

b. refractoriness increase M2

c. automaticity decrease M2

 

4. ventricle (only effects on contractility)

a. conduction nothing 

b. refractoriness nothing

c. automaticity nothing

d. contractility decrease M2

 

Term
ACH has inhibitory effects on which receptor? and which neuron terminals?
Definition
receptor M2 neuron terminals: adrenergic and cholinergic
Term
Norepinephrine has inhibitor effects on which receptor and which nueron terminals?
Definition
receptor: alpha 2 neuron terminals: adrenergic and cholinergic
Term
Norepinephrine has inhibitor effects on which receptor and which nueron terminals?
Definition
receptor: alpha 2
neuron terminals: adrenergic and cholinergic
Term
epinephrine has excitatory effects on which receptor and which neuron terminals?
Definition
beta 2 receptors for adrenergic and somatic motor cholinergic neuron terminals.
Term
what are three mechanisms for indirect adrenergic drugs?
Definition
1. facilitated exchange diffusion
2. false transmitter concept
3. inhibition of reuptake of catecholamines that are already released
Term
effects of SNS on fat cells and the accompanying receptors?
Definition
increased lipolysis Beta 3
decreased lipolysis alpha 2
Term
effects of SNS on platelets and the accompanying receptor?
Definition
aggregation - alpha 2
Term
effect of SNS on mast cells, basophils and the accompanying receptor?
Definition
inhibition of granulation -Beta 2
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