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25 Cards in this Set

  • Front
  • Back

What do local anaesthetics act on?

local anaesthetics inhibitnerve conduction byblocking sodium channels

What are the features of SYMPATHETIC NERVES?

Pre Ganglionic fibres short, close to CNS. Large distance between pre and post ganglionic elements

What are the features of the Parasympathetic nerves?

Pre ganglionic fibres closer to target tissues

What are the features of the MOTOR NERVE?

Goes to Neuromuscularjunction (NMJ,skeletal muscle)

Where is noardrenaline neurotransmitter found?

Noradrenaline (NA) – sympathetic terminals

Where is ACh found?

Acetylcholine (ACh) – parasympatheticterminals, ganglia& NMJ

Where is Dopamine found?

Dopamine (DA) – parts of CNS

Where is serotonin found?

Serotonin (5-HT) – parts of CNS

Where is Nitric oxide (NO) found?

Various, erectile tissue in particular

What is the Anatomy of sympathetic nervoussystem?

Emanates fromTHORACOLUMBARsegments of spinal cord


Ganglia –Typically close to spinalcord in the paravertebralchain

What is the Anatomy of parasympathetictransmission?

TWO IMPORTANT POINTS


Craniosacral outflow……


(i) Cranial – oculomotor,facial, glossopharyngeal,vagal


(ii) Sacral – nervi erigentes


Ganglia –Close to orinside target tissues

What happens at the The neuroeffector junction (terminal region)?

Ation potential ----> depolarisation


----> voltage operatedcalcium channel ---->NT release ----> postsynapticagonism -----> presynapticautoinhibitoryagonism

What drugs act on the Synthesis and storage of transmitter?

INHIBITORY EFFECTS


precursor uptake(ACh x by hemicholinium)enzyme cascade(NA x by AMPT)


Storage(NA x by reserpine)


STIMULATORY EFFECTS


provide excessprecursor(L-DOPA/DA)

What is L-DOPA used to treat?

Major Therapeutics: L-DOPA to increasedopamine levels in the brains of patients withParkinson’s disease

What drugs affect the Release of transmitter?

INHIBITION


Inhibit terminal depolarisation(NA x by guanethidine; ofminor importance to itsoverall effect)


(Ca entry by conotoxin)


vesicle fusion(ACh x by Botulinum)


presynaptic receptor(NA x by clonidine - α2 adrenergic agonist )


STIMULATION


displace NT(NA: byamphetamine andguanethidine)

What drugs act on Termination of neurotransmission?

INHIBITION OF TERMINATION


(Note that inhibition oftermination willenhance transmission)


inhibit reuptake(NA/cocaine;5-HT/fluoxetine)


inhibit enzyme(neostigmine/ACh)

What are the mahor therapeutic effects of Prozac?

Major therapeutics: tricyclic antidepressantsinhibit NA uptake; fluoxetine(Prozac) inhibits 5-HT uptake

What are the major therapeutic effects of anticholinesterases?

Major therapeutics:anticholinesterases to reversemuscle relaxation in surgery

What is Agonist and antagonist action on receptors?

Agonist:affinity and efficacystimulate receptormimic transmitter


Antagonist:affinity but no efficacyblock binding siteinhibit transmitter

What are the Receptor agonists with majortherapeutic applications?

Transmitter/Receptor Drug Use


Noradrenaline/β2 - salbutamol asthmaNoradrenaline/α1 - phenylephrine decongestantDopamine/D2 - bromocriptine - Parkinson’s Disease


Enkephalin/µ - morphine - pain relief


GABA/A - diazepam - anxiety

What should be noted about diazepam?

(note diazepam acts on a site different on the receptor from the GABA bindingsite to enhance the effects of GABA – not strictly an agonist)

What are the Receptor antagonists with majortherapeutic applications?

Transmitter/Receptor Drug UseNoradrenaline/α1 - prazosin - reduce BPNoradrenaline/β - propranolol - reduce BPAcetylcholine/nicotinic - atracurium muscle relaxant


Acetylcholine/muscarinic - atropine - pre-medDopamine/D2 - trifluoperazine - antipsychotic

What are some Drugs affecting the neuroeffector response?

Benzodiazepine tranquillisers:


Bind to the GABA receptor/Cl ionchannel complex to enhancechannel opening and potentiateinhibitory effects of GABA


Sildenafil (Viagra):


Inhibits breakdown of thesecond messenger substancecyclic GMP produced by nitricoxide in erectile tissue

What are the sites of drug action?

1. synthesis


2. storage


3. release


4. receptors


5. cessation

Why is the synapse is an important target for drug action?

The synapse is an important target for drug action because:


• it is the site of neurotransmission


• it is the site where the transmitter is synthesised, stored andreleased


• it is a major location for receptors and target for agonists orantagonists


• receptors offer the best chance of producing drugs with ahigh degree of selectivity and therefore with reduced sideeffect profile