SNS Flashcards
What is the SNS response?
Mydriasis
Decreased salivation
Increased HR, SV
Vasoconstriction
Bronchodilation and decreased lung secretions
Reduced GI motility and secretions
Inhibition of bladder contraction
Glycogenolysis
Which are the Adrenergic Receptors
Alpha: a1 and a1
Beta: B1, B2, B3
In which 2 places do the SNS neurons behave differently
Adrenal medulla: where NE–>E by Phenylethanolamine N methyl transferase
Sweat glands: ACh is neurotransmitter
Which enzymes metabolise NE and E
COMT: catechol-o-methyl transferase
MAO: monoamine oxidases
Steps in NE neurotransmission
- Hydroxylation of tyrosine
- Dopamine enters vesicle and is converted to NE
- Influx of Ca causes release of NE via exocytosis
- Binding of NE to postsynaptic receptor activates the receptor
- Released NE is rapidly taken into neuron.
- NE is metabolised by MAO and COMT
What inhibits re-uptake of NE?
Cocaine and Imipramine
NE acts on which receptors
a1, a2, B2 and its direct acting
E acts on which receptors
a1,a2,B1,B2 and its direct acting
Ephedrine acts on which receptors
its acts on all adrenergic receptors both direct and indirect acting by weakly stimulating the release of NE and E from nerve endings in SNS
Amphetamine causes…
strong NE and E release indirectly
Cocaine causes
Directly inhibits NE and Dopamine re-uptake
a1 receptors are located…
on post synaptic membrane
a1 receptors are specific to
vascular smooth muscle
Eye
a2 receptors are located…
Presynaptic nerve endings
a2 receptors are specific to
GIT, pancreas and platelets
They inhibit release of NE
Which alpha receptors is stimulatory and which is inhibitory
a1: stimulatory
a2: inhibitory
B1 receptor is specific to
Cardiac tissue
B2 receptor is specific to
Respiratory, uterus, Liver, VSM
B3 receptors are specific to
Detrusor muscle of bladder
are involved in Lipolysis
Adrenergic receptors have affinity for which neurotransmitter
a1: NE > E
a2: E > NE
B1: NE=E
B2: E»NE
Response of a1 stimulation
Vasoconstriction
Incr. Peripheral Resistance
Incr. BP
Mydriasis
Incr closure of bladder sphincter
Response of a2 stimulation
Inhibits NE release
Incr. Acetylcholine release
Inhibition of insulin release
Response of B1 stimulation
Incr HR
Incr. Lipolysis
Incr. Myocardial contractility
Incr. Renin
Response of B2 stimulation
Vasodilation
Decr. Peripheral Resistance
Bronchodilation
Incr. Glycogenolysis
Incr. Glucagon release
Relaxes uterine smooth muscle
Indications of Adrenaline
Drug of choice in Anaphylaxis
Combined with LA=incr. DOA
During cardiac arrest
CI of Adrenaline
Tachyarrythmias
Pheochromocytoma
Administration of Adrenaline
IM,SC
IV in severe cases
A/E of adrenaline
peripheral vasoconstriction: prolonged use can cause necrosis/gangrene
Angina
hypertension
Tachycardia
Ventricular arrythmias
MOA of Adrenaline
Potent stimulant of a and B adrenoreceptors
Potent vasoconstrictor and cardiac stimulant
+ve inotropic & chronotropic actions on heart ( β1)
vasoconstriction in vascular beds (α)
Also activates β2 receptors in skeletal muscles vasodilation
Respiratory : bronchodilation (β2)
Hyperglycemia : increased glycogenolysis in liver (β2) decreased
release of insulin (α2)
Phenylephrine is a
A1 agonist
MOA of Phenylephrine
Vasoconstrictor= Incr BP
Causes mydriasis
Vasoconstriction of nasal mucosa= decreased nasal secretions
Indications of Phenylephrine
Nasal decongestant
Hypotension
Mydriatic in Eye exams
Administration of Phenylephrine
Oral, topical
IV
Eye drops
A/E of Phenylephrine
Nausea
Hypertension
Oxymetazoline and Xylometazoline are
Alpha adrenergic agonists
Administration of Oxymetazoline and Xylometazoline
Topical nasal sprays
MOA of Oxymetazoline and Xylometazoline
Vasoconstrict nasal mucosa and conjunctiva
Indications of Oxymetazoline and Xylometazoline
Nasal decongestant
How long can Oxymetazoline and Xylometazoline be used
Max. 5 days
>5 days: Rebound congestions
Clonidine is
a2 adrenoreceptor in CNS
Indications of Clonidine
Migraine prophylaxis
a-metyldopa is
a2 agonist in brain
MOA of a-methyldopa
decr. sympathetic outflow= decr HR, decr. CO and TPR= Decr. BP
Indications of a-methyldopa
Hypertension in pregnancy
A/E of a-methyldopa
Sedation
Hyperprolactinaemia
Dopamine is
immediate metabolic precursor of NE
a and B agonist
D1 and D2 agonist(dopaminergic)
Low dose of dopamine causes
activation of dopaminergic Rs in renal vessel–> incr. cAMP= renal vasodilation and diuresis
Higher dose of dopamine cause
acts on B1in heart: +ive chronotopic and -ive iontropic effects on myocardium=
incr. HR and contractility (incr. SV)
Large doses of Dopamine cause
a1 adrenoreceptor activation
=vasoconstriction
Indications of Dopamine
Shock treatment
Severe HF
Acute Hypotension
A/E of Dopamine
Nausea
Hypertension
Arrythmians
Dobutamine is a
B1 selective agonist
MOA of Dobutamine
Causes +ive inotropic effects
= Incr. CO
Indications of Dobutamine
Acute MI
A/E of Dobutamine
Atrial Fibrilation
Which are the short-acting B2 agonists
Salbutamol
Fenoterol
Terbutaline
Which are the long-acting B2 agonists
Salmeterol
Formoterol
Which are the ultra-long acting B2 agonists
Indacaterol
Vilanterol
MOA of B2 agonists
bronchodilation- relaxes bronchial SM
Indications of B2 agonists
Asthma
COPD
Administration of B2 agonists
Inhaler
A/E of Salbutamol and Salmeterol
Restlessness
Tremor
Tachycardia or arrythmia
Indication of Ephedrine
Treatment of Hypotension
DOA of Ephedrine
Long DOA
What does Ephedrine do to CNS
Causes a mild stimulant effect
Administration of Ephedrine
IV
Etilefrine is a
a and B agonist
Administration of Etilefrine
IV
Indications of Etilefrine
Treats hypotension
Pseudephedrine is a
mainly a1 agonist
lesser B2 agonist
Indications of Pseudoephedrine
Systemic nasal decongestant
Administration of Pseudoephedrine
Oral
A/E of Pseudoephedrine
CNS stimulation with anxiety
Restlessness
Tremor
Hypertension
Tachycardia
Palpitation
Selective a1 blockers are
Prazosin
Doxazosin
Tamulosin
Terazosin
Non-selective a blockers
Reversible: Phentolamine
Irreversible: Phenoxybenzamine
Indications of Phenoxybenzamine
Pheochromocytoma (pre-op)
Raynaud disease
A/E of Phenoxybenzamine
Postural Hypotension
nasal stuffiness
Nausea and vomiting
Decr. ejaculation
CI of Phenoxybenzamine
CV disease
Indications of Phentolamine
Pheochromocytoma
HPT crisis
(MAO I tyramine food, Clonidine withdrawal)
A/E of Phentolamine
Postural Hypotension
Arrythmias
Angina pain
CI of Phentolamine
IHD: Ischemic Heart Disease
Indications of Prazosin, Terazosin, Doxazosin
Hypertension
BPH
A/E of a1 selective blockers
Postural Hypotension
Headache
Drowsiness
Nasal Congestion
Selective a1a blockers are
Tamulosin
Alfuzosin
Indications of a1a blockers
BPH: drugs of choice
A/E of a1a blockers
Retrograde ejaculation
Floppy eye syndrome
DOA of phenoxybenzamine
24hrs
DOA of phentolamine
4hrs
DOA of Prazosin
short doa
T1/2 of selective a-blockers
Prazosin: 3hrs
Terazosin: 9-12hrs
Tamsulosin: 9-15hrs
Doxazosin: 22hrs
A1 receptor antagonism results is
Arteriolar dilation=decr. afterload
Venous dilation=decr. preload–> decr. VR
Prazosin and its analogues act
at vascular SM and prostate
Tamsulosin acts
Selectively at prostate
B1 Blocker effects are
decr. HR
Incr. AV conduction
decr. CO
decr. O2 consumption
decr. BP
decr. Renin
decr. aqueaous humour
B2 Blocker effects are
incr. airway resistance
Arterial vasoconstriction
decr. Gluconeogenesis
decr. Glycogenolysis
decr. tremors
Selective B1 blockers are
Atenolol
Bisoprolol
Metaprolol
Nebivolol
Esmolol
Non-selective B-blockers are
Propranolol
Timolol
B1,B2 and a1 blockers are
Carvedilol
Labetolol
Indications of Propranolol
Hypertension
Migraine
Hyperthyroidism
Angina pectoris
MI
Indications of Timolol
Glaucoma
Hypertension
Indications of B1 blockers (know which ones)
Hypertension
Angina
Acute MI: Atenolol
CHF: Bisoprolol+ACE1+diuretics
Indication of Nebivolol
Hypertension
Indications of B1,B2 and a1 blockers
Hypertension
Non-acute Congestive HF
S/E of B-blockers
Bronchospasm: B2
Bradycardia: All
Heart block/HF: All
Fatigue
Impotence in males
Hypoglycaemia: B2
Cold extremities: B2
Vivid dreams
CI of Beta blockers
Asthma/COPD
Diabetics
LVHF, Cardiogenic shock
SInus Bradycardia
TU of Propranolol
HT
Migraine prevention
Hyperthyroidism: thyrotoxicosis
Angina
MI
Essential Tremor
Anxiety symptoms
MOA of Timolol
Decreases intraocular pressure in glaucoma by decr. secretion of aqueous humour of ciliary body
MOA of Bisoprolol, Atenolol,Metoprolol
Reduce HR, CO
Decr. O2 demand and workload
SLow AV conduction
Reduces Renin release from JG cells
MOA of B1, B2 and a1 blocker
Peripheral vasodilation= decr. BP
Reduce afterload, contractility and O2 demand