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ANS
Pharm I - Block 2
58
Pharmacology
Not Applicable
06/07/2010

Additional Pharmacology Flashcards

 


 

Cards

Term

Ganglionic level neurotransmitter for

Symp

&

Parasymp

Definition
Ach 
Term

post ganglionic pre synaptic neurotransmitters

 

Symp

&

Parasymp

Definition

Symp - Norepi

 

Parasymo - Ach

Term
Cholinergic/ parasympathetic receptors
Definition
M1, M2, M3, Nm & Nn
Term
Sympathetic Receptors
Definition
A1, A2, B1, B2 & B3
Term
Gq coupled & response
Definition

M1, M3 & A1

 

PLC

 

IP3 (increase in ca2+) - DAG (protein kinase C)

Term
Gi coupled & response
Definition

M2 & A2

 

Decrease in Adenylyl Cyclase

 

Decrease in cAMP - Decrease in protein Kinase A

Term
Gs coupled & response
Definition

B1, B2 & B3

 

Increase Adenylyl Cyclase

 

Increase cAMP

 

Increase Protein Kinase A

Term

M2

coupled & response

Definition

Gi 

 Decrease in AC

Decrease in cAMP

Decrease in HR

 

Term

M3

coupled & response

Definition

Gq

PLC & IP3-DAG

smooth muscle contraction and gland secretion ...

Urination, bronchospasm, lacrimation

Pupil constriction - Miosis thus increased flow of AH

Term

B1

Coupled & response

Definition

Gs

Increase in AC & cAMP

Increases HR

Term

B2

coupled & response

Definition

Gs

Increase in AC & cAMP

smooth sucle relaxation 

bronchodilation, urinary retention, uterus relaxation

Term

B3

coupled & response

Definition

Gs

Increase in AC & cAMP

Fat lipolysis

Term

A1

coupled & response

Definition

Gq

PLC & IP3 - DAG

VASOCONSTRICION

*** remember if you want to vasodilate you have to block this receptor!*

Pupil dilation (mydriasis)

 

Term

A2

coupled & response

Definition

Gi 

Decrease in AC & cAMP

Reduces the release of Norepi leading to bradycardia

Decreased insulin release

Term
Cholinergic/parasympathetic neurotransmission is terminated by?
Definition
AchE
Term
Andrenergic/sympathetic neurotransmission is terminated by
Definition
reuptake
Term
Ways in which Ach (cholinergic/parasympathetic transmission) is blocked
Definition

1.Hemicholinium stops initial choline from being transformed into acetyl-CoA+Choline

2.Blocked from going in to mobile via vesamicol

3.Vesicle blocked from docking via botulimoum

Term
Ways in which adrenergic (sympathetic transmission) is blocked
Definition

1.Metyrosine blocks tyrosine from converting to DOPA

2.Stopped from entering the mobile poos via reserpine

3. Vesicle blocked from docking via bretylium & guanethidine (increases docking via amphetamine)

4. Block Re-uptake pump via amphetamine, cocaine and TCA's

Term
how does Ach cause Vasodilation?
Definition

binds to endothelium of the blood vessel releasing NO.. ONLY

if endothelium layer is intact

Term
Direct acting cholinergic agonists
Definition

•Bethanechol
•Pilocarpine (naturally occurring alkaloid)
•Carbachol
•Methcholine

Term
Indirect acting cholinergic agonists
Definition

•Neostigmine,
•Physostigmine
•Pyridostigmine
•Edrophonium
•Tacrine ,Danopezil
•Ecothiophate
•Malathion,Parathion
•Sarin

Term
Vasodilation via Ach
Definition

Vasodilatation  by ACh is due to the release of EDRF (Endothelium Derived Relaxing Factor) which is nothing but Nitric Oxide 

Term

Bethancol 

1. class of drug

2. Uses

Definition

1. Direct acting cholinergic agonist

2. Paralitic ileius

2. Atony of the Bladder

Term
symptoms of paralytic ileus
Definition

Paralytic ileus : It is the condition characterised by reduced bowel movements, inability to pass stools or flatus. Typically seen in postoperative patients.   

Term

Symptoms of Atony of the bladder

how is it treated?

Definition

non obstructive urinary retention, usually seen in patients with neurological problems and post opp. patients

 

By stimulating M3 receptors bethanechol increases the bowel movements and bladder contractions facilitates 

Term

Pilocarpine

1. class of drug

2. Uses

Definition

1. Directs acting cholinergic agonist

2. Glaucoma & Sjogrens syndrome

 

** lipid soluble and penetrates the cornea very well**

Term

Sjogrens syndrome sympotoms

how is it treated?

Definition

Sjogren's syndrome aka is a chronic, inflammatory, autoimmune disorder characterised by dry mouth (xerostomia) and dry eyes (keratoconjuctivitis sicca) - due to the distruction of the lacrimal and salivary glands
can cause Mikulicz syndrome - enlargement of the salivary & lacrimal glands

often associated with Rheumatoid arthritis, parotid enlargement & increased risk of B-cell lymphoma and other autoimmune disorders - antiribonucleoprotein antibodies - SS-A (Ro) & SS-B (La)
Pilocarpine a direct acting cholinergic agonist is used to treat the symptoms  (dry eyes & mouth)

 

Term

How do indirect acting cholinergic agonists work?

what are the classes of indirect acting cholinergic agonists?

Definition

1. They block the AchE enzyme from breaking down Ach at the synaptic cleft, thus increasing the amount of Ach avaliable

2.There are reversible and irreversible types

Term
Name the reversible indirect acting cholinergic agonists
Definition

Neostigmine

Physostigmine

Pyridostigmine

Edrophonium

Tacrine

Danopezil

Term
Name the irreversible indirect acting cholinergic agonists
Definition

Ecothiophate

Malathion

Parathion

Sarin

Term
symptoms of myasthenia gravis
Definition

Typical symptom is  transient weakness. Frequent findings are ptosis, diplopia, difficulty in speaking and swallowing, and extremity weakness. Severe disease may affect all the muscles, including those necessary for respiration.

Term
what is used in the management of myasthenia gravis?
Definition

reversible indirect acting cholinergic agonists

 

–Neostigmine
–Pyridostigmine
–Edrophonium

 

Term

Neostegmine

1.class of drug

2.use

Definition

1. reversible indirect acting cholinergic agonist

2. Acute cases of MG - given via IV

Term

Phyridostegmine

1. Class of drug?

2. Use

Definition

1. Indirect acting reversible cholinergic agonist

2. longer duration that nenostegmine, thus given for long term/ maintenance - given orally

Term

Edrophonium

1. Class of drug

2. Use

Definition

1. Reversible indirect acting cholinergic agonist

2. Shortest duration of action (5 mins) thus used in the Tensilon test to check for MG - differentiate cholinergic crisis (excessive drug therapy) from myashtenic crisis (insufficient medication)

Term
What is the difference between MG and Eaton-Lambert syndrome
Definition

MG is an autoimmune disease with autoantibodies directed against post synaptic Ach receptors - WEAKNESS WORSENS WITH REPEATED CONTRACTIONS - associated with thymic hyperplasia and thymomas

 

Eaton-Lambert syndrome - autoantibodies directed against the presynaptic calcium channels  leads to a decrease in ACh release - extra-occular muscles are spared - WEAKNESS IMPROVES WITH REPEATED CONTRACTION - commonly a paraneplastic syndrome of small cell lung cancer

Term
tensilon test results
Definition

in the case of Mg - patient will get better

in pt with cholinergic crisis the pt will get worse

Term
What do you administer when the tensilon test is administered and the pt gets worse?
Definition
you must give atropine which is an anticholinergic
Term
What drugs are used for Alzheimer's & why?
Definition

Tacrine,

Rivastigmine

Donepezil

& NMDA antagonists - Memantine (blocks glutamate at the NMDA receptors)

They cross the bbb

Term
What is the only irreversible indirect acting cholinergic antagonist that is used medically?
Definition
Ecothiophate - long acting drug used in glucoma
Term

symptoms of OP poisioning

what is responsible for these symptoms?

Definition

miosis, blurred vision, bradycardia ,salivation, sweating, urination (urinary incontinence), bronchial constriction, vomiting, and diarrhea.

 

Phosphorylation (irreversible inhibition ) ofthe enzyme resulting in excess acetylcholine 

Term

what is the sign that enough atropine has been adminstered?

when is it administered?

Definition

dilated pupils

 

given immediately when OP poisoning has occured

Term

What is given to treat OP poisoning after atropine is immediately given?

 

what is the condition of the use of the drug?

Definition

Parlidoxamine - which is an AchE activator that acts by hydrolysing the drug bound enzyme

 

it must be given before the enzyme has 'aged' - this is when the interaction between the drug and the enzyme is irreversible

Term

Anticholinergics - refer to

NMJ blockers/ skeletal muscle relaxants- refer to

Definition

muscarenic blockers

nicotinic blockers

Term

Atropine

1. class of drug

2.action

Definition

1. anticholinergic

2. crosses BBB

pupillary dilation & cycloplegia - loss of accommodation reflex thus blurred vision

dry mouth

tachycardia

bronchodilation

constipation

urinary retention

excitation/hallucinations

Term
What kind of patient should anticholinergics not be administered?
Definition

Elderly

BPH patients

Hyperthermic infants

Term

Tropicamide

1. class of drug

2. Use

Definition

1. Anticholinergic

2. short acting (4 hours) produces mydraisis and cycloplegia - for refractive error testing fundoscopy

Term

Benztropine

1. class of drug

2. use

Definition

1. anticholinergic

2. Used in drug induced Parkinsonism to treat EPS symptoms

Term

Ipratropium bromide
1. class of drug
2. use

 

Definition

1. anticholinergic

2. COPD /Bronchial asthma (not much systemic  absorption, so less side effects)

due to bronchodilation as it blocks M receptors

Term

Meth scopolamine or propantheline 
1. class of drug
2. use

 

Definition

1. anticholinergic

2.to treat peptic ulcers - as it reduces the secretions in GI

Term

Scopolamine 

1. Class of drug

2. Use

Definition

1. anticholinergic

2.to prevent Motion sickness 

Term

Dicyclomine  

1. class of drug

2. use

Definition

1. anticholinergic

2. to treat GI spasm, spamodicabdominal pain Eg: Menstrual pain or renal colic

Term

Glycopyrrolate: 
1. class of drug
2. Use

Definition

1. Anticholinergic

2. used in GA to reduce bronchial secretions (before intubation)

Term

Oxybutynin

 

Class of drug?

 

Use?

Definition

Anticholinergic/antimuscurenic/ muscurenic antagonist

 

Reduce urgency in mild cystitis and reduce bladder spasms

Term

Hexamethonium

 

Class of drug?

 

Use?

 

ADR?

Definition

Nicotinic antagonist - Ganglionic blocker

 

Used in experimental models to prevent vagal reflex responses to changes in blood pressure - eg prevents reflex bradycardia caused by NE

 

Orthostatic Hypotension

Blurred vision

Constipation

Sexual dysfunction

Term

What is given in an atropine OD?

Class of drug?

Definition

Physiostegmine

 

Indirect acting cholinergic

 

also used in glucoma

Term

Carbacol

 

Class of drug?

Use?

 

Definition

direct acting cholinergic

 

Glaucoma - Miosis and release of intraocular pressure

Term

Methcholine

 

Class of drug?

Use?

Definition

Direct acting cholinergic

 

Challenge test for diagnosis of asthma

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