Pharmacology of the Sympathetic Nervous System I & II Flashcards by XXXXX _

Q

Class

Noradrenaline (alpha effects)

A

Class:

Adrenoceptor Agonist

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Q

Uses (treatments)

Noradrenaline (alpha effects)

A

Uses:

No clinical use (despite being more potent than Adrenaline)

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Q

Mechanism

Noradrenaline (alpha effects)

A

Mechanism:

alpha & beta action
Alpha1 –> phospholipase C activation –> IP3 & DAG formation –> increase in calcium release
Alpha2 –> inhibit adenylate cyclase –> decrease cAMP –> decrease Protein Kinase A (PKA)

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Q

Action

Noradrenaline (alpha effects)

A

Action:

alpha1 –> smooth muscle contraction, vasoconstriction, decrease GI motility, promote glycogenolysis
alpha2 –> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

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Q

Side Effects (+ special features)

Noradrenaline (alpha effects)

A

Side Effects & Special Features:

Hypertension
Reflex bradycardia
Vasoconstriction (activation of alpha-receptors)

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Q

Class

Noradrenaline (beta effects)

A

Class:

Adrenoceptor Agonist

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Q

Uses (treatments)

Noradrenaline (beta effects)

A

Uses:

No clinical use
(Less potent than adrenoceptors in beta action)
Treatment of asthma
Inhibition of pre-term labour
Treatment of acute congestive heart failure

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Q

Mechanism

Noradrenaline (beta effects)

A

Mechanism:

alpha (more) & beta (less) action
Increased cAMP
Activation of Protein Kinase A (PKA) –> leads to protein phosphorylation
Prolonged opening of calcium channels in the heart (Beta 1)

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Q

Action

Noradrenaline (beta effects)

A

Action:

beta1 –> Increase heart rate & contractile force, vasodilation, renin release, inhibition of histamine, increased glycogenolysis & lipolysis
beta2 –> smooth muscle relaxation (bronchodilation), smooth muscle vasodilation
beta3 –> thermogenesis

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Q

Side Effects (+ special features)

Noradrenaline (beta effects)

A

Side Effects & Special Features:

Hypokalaemia
Tremor
Hypotension
Reflex tachycardia

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Q

Class

Adrenaline (alpha effects)

A

Class:

Adrenoceptor Agonist (alpha effects)

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Q

Uses (treatments)

Adrenaline (alpha effects)

A

Uses:

Less potent than NA (but clinically used unlike NA)
Anaphylactic shock (epipens)
Cardiac arrest
Prolong action of local anaesthetics

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Q

Mechanism

Adrenaline (alpha effects)

A

Mechanism:

alpha & beta action
Alpha1 –> phospholipase C activation –> IP3 & DAG formation –> increase in calcium release
Alpha2 –> inhibit adenylate cyclase –> decrease cAMP –> decrease Protein Kinase A (PKA)

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Q

Action

Adrenaline (alpha effects)

A

Action:

alpha1 –> smooth muscle contraction, vasoconstriction, decrease GI motility, promote glycogenolysis
alpha2 –> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

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Q

Side Effects (+ special features)

Adrenaline (alpha effects)

A

Side Effects & Special Features:

Hypertension
Reflex bradycardia
Vasoconstriction (activation of alpha-receptors)
High Dose given –> to overcome smooth muscle vessel vasodilation (beta 2 induced)
Activates alpha receptor to cause vasoconstriction

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Q

Class

Isoprenaline

Alpha or beta effect?

A

Class:

Adrenoceptor Agonist (strong beta effects - weak alpha effects)

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Q

Uses (treatments)

Isoprenaline

Alpha or beta effect?

A

Uses:

Treatment of asthma
Inhibition of pre-term labour
Treatment of acute congestive heart failure

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Q

Mechanism

Isoprenaline

Alpha or beta effect?

A

Mechanism:

Increased cAMP
Activation of Protein Kinase A (PKA) –> leads to protein phosphorylation
Prolonged opening of calcium channels in the heart (Beta 1)

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Q

Action

Isoprenaline

Alpha or beta effect?

A

Action:

beta1 –> Increase heart rate & contractile force, vasodilation, renin release, inhibition of histamine, increased glycogenolysis & lipolysis
beta2 –> smooth muscle relaxation (bronchodilation), smooth muscle vasodilation
beta3 –> thermogenesis

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Q

Side Effects (+ special features)

Isoprenaline

Alpha or beta effect?

A

Side Effects & Special Features:

Hypokalaemia
Tremor
Hypotension
Reflex tachycardia

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Q

Class

Phenylephrine

Alpha or beta effect? (predominantely)

A

Class:

Adrenoceptor Agonist (alpha effect mainly)

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Q

Uses (treatments)

Phenylephrine

Alpha or beta effect? (predominantely)

A

Uses:

Targets alpha1 –> causing BP Increase + Reflex Bradycardia
Nasal decongestant (vasoconstricts capillaries)

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Q

Mechanism

Phenylephrine

Alpha or beta effect? (predominantely)

A

Mechanism:

alpha1 –> phospholipase C activation –> IP3 & DAG formation –> increase in calcium release
alpha2 –> inhibit adenylate cyclase –> decrease cAMP –> decrease Protein Kinase A (PKA)

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Q

Action

Phenylephrine

Alpha or beta effect? (predominantely)

A

Action:

alpha1 –> smooth muscle contraction, vasoconstriction, decrease GI motility, promote glycogenolysis
alpha2 –> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

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Q

Side Effects (+ special features)

Phenylephrine

Alpha or beta effect? (predominantely)

A

Side Effects & Special Features:

Hypertension
Reflex bradycardia
Vasoconstriction (activation of alpha-receptors)

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Q

Class

Clonidine

Specific target?

A

Class:

Adrenoceptor Agonist (alpha2 target)

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Q

Uses (treatments)

Clonidine

Specific target?

A

Uses:

Imidazoline receptor agonist (CNS) –> anti-hypertensive, anxiolytic, attention deficit, hyperactivity, withdrawal

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Q

Mechanism

Clonidine

Specific target?

A

Mechanism:

alpha2 –> inhibit adenylate cyclase –> decrease cAMP –> decrease Protein Kinase A (PKA)

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Q

Action

Clonidine

Specific target?

A

Action:

alpha2 –> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

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Q

Side Effects (+ special features)

Clonidine

Specific target?

A

Side Effects & Special Features:

Hypertension (probably not)
Reflex bradycardia (probably not)
Vasoconstriction (activation of alpha-receptors)

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Q

Class

Brimonidine

A

Class:

Adrenoceptor Agonist (alpha2)

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Q

Uses (treatments)

Brimonidine

A

Uses:

Treatment of open angle glaucoma

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Q

Mechanism

Brimonidine

A

Mechanism:

alpha2 –> inhibit adenylate cyclase –> decrease cAMP –> decrease Protein Kinase A (PKA)

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Q

Action

Brimonidine

A

Action:

alpha2 –> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

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Q

Side Effects (+ special features)

Brimonidine

A

Side Effects & Special Features:

Hypertension (probably not)
Reflex bradycardia (probably not)
Vasoconstriction (activation of alpha-receptors)

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Q

Class

alpha-methylnoradrenaline

A

Central-acting alpha 2 agonists

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Q

Class

Salbutamol

Specific effect on?

A

Class:

Adrenoceptor Agonist (beta 2 receptors)

Uses:

Treatment of asthma
Inhibition of pre-term labour
Treatment of acute congestive heart failure

Mechanism:

Increased cAMP
Activation of Protein Kinase A (PKA) –> leads to protein phosphorylation

Action:

beta2 –> smooth muscle relaxation (bronchodilation), smooth muscle vasodilation

Side Effects & Special Features:

Hypokalaemia
Tremor
Hypotension
Reflex tachycardia

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Q

Uses (treatments)

Salbutamol

Specific effect on?

A

Uses:

Treatment of asthma
Inhibition of pre-term labour
Treatment of acute congestive heart failure

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Q

Mechanism

Salbutamol

Specific effect on?

A

Mechanism:

Increased cAMP
Activation of Protein Kinase A (PKA) –> leads to protein phosphorylation

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Q

Action

Salbutamol

Specific effect on?

A

Action:

beta2 –> smooth muscle relaxation (bronchodilation), smooth muscle vasodilation

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Q

Side Effects (+ special features)

Salbutamol

Specific effect on?

A

Side Effects & Special Features:

Hypokalaemia
Tremor
Hypotension
Reflex tachycardia

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Q

Class

Dobutamine

Specific effect on?

A

Class:

Adrenoceptor Agonist (beta 1 receptor effect)

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Q

Uses (treatments)

Dobutamine

Specific effect on?

A

Uses:

Emergencies –> to create positive inotropic action (contraction)
Treatment of asthma
Inhibition of pre-term labour
Treatment of acute congestive heart failure

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Q

Mechanism

Dobutamine

Specific effect on?

A

Mechanism:

Increased cAMP
Activation of Protein Kinase A (PKA) –> leads to protein phosphorylation
Prolonged opening of calcium channels in the heart (Beta 1)

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Q

Action

Dobutamine

Specific effect on?

A

Action:

beta1 –> Increase heart rate & contractile force, vasodilation, renin release, inhibition of histamine, increased glycogenolysis & lipolysis

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Q

Side Effects (+ special features)

Dobutamine

Specific effect on?

A

Side Effects & Special Features:

Hypokalaemia
Tremor
Hypotension
Reflex tachycardia

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Q

Class

Phentolamine

A

Class:

alpha-adrenoceptor antagonist

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Q

Uses (treatments)

Phentolamine

A

Uses:

Reversible
Anti-Hypertensive
Treatment of phaeochromocytoma (to decrease BP)
Reverse of dental local anaesthesia

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Q

Mechanism

Phentolamine

A

Mechanism:

Block alpha-adrenoceptor mediated effects by direct competition

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Q

Action

Phentolamine

A

Action:

Increased sympathetic drive (indirect - reflex)
Vasodilation
Decreased BP

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Q

Side Effects (+ special features)

Phentolamine

A

Side Effects & Special Features:

Nasal stuffiness (due to vasodilation)
Reflex tachycardia
Postural hypotension
Sodium & water retention
Miosis (pupillary constriction)

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Q

Class

Phenoxybenzamine

A

Class:

alpha-adrenoceptor antagonist

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Q

Uses (treatments)

Phenoxybenzamine

A

Uses:

Irreversible
(Possible) Male constraceptive
Anti-hypertensive
Treatment of phaeochromocytoma (to decrease BP)
Reverse of dental local anaesthesia

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Q

Mechanism

Phenoxybenzamine

A

Mechanism:

Block alpha-adrenoceptor mediated effects by non-competitive & irreversible inhibition

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Q

Action

Phenoxybenzamine

A

Action:

Increased sympathetic drive (indirect - reflex)
Vasodilation
Decreased BP

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Q

Side Effects (+ special features)

Phenoxybenzamine

A

Side Effects & Special Features:

Nasal stuffiness (due to vasodilation)
Reflex tachycardia
Postural hypotension
Sodium & water retention
Miosis (pupillary constriction)

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Q

Class

Prazosin

Selective for?

A

Class:

alpha-adrenoceptor antagonist (alpha1 selective)

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Q

Uses (treatments)

Prazosin

Selective for?

A

Uses:

Decrease BP
Anxiety
PTSD
Short-acting
Decrease urinary retention
Allow kidney stone passage
Anti-hypertensive
Treatment of phaeochromocytoma (to decrease BP)
Reverse of dental local anaesthesia

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Q

Mechanism

Prazosin

Selective for?

A

Mechanism:

Block alpha-adrenoceptor mediated effects by direct competition

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Q

Action

Prazosin

Selective for?

A

Action:

Increased sympathetic drive (indirect - reflex)
Vasodilation
Decreased BP

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Q

Side Effects (+ special features)

Prazosin

Selective for?

A

Side Effects & Special Features:

Nasal stuffiness (due to vasodilation)
Reflex tachycardia
Postural hypotension
Sodium & water retention
Miosis (pupillary constriction)

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Q

Class

Doxazosin

Selective for?

A

Class:

alpha-adrenoceptor antagonist (alpha1 selective)

Q

Uses (treatments)

Doxazosin

Selective for?

A

Uses:

Long-acting
Better for BP Control
Decrease BP
Decrease urinary retention
Allow kidney stone passage
Anti-hypertensive
Treatment of phaeochromocytoma (to decrease BP)
Reverse of dental local anaesthesia

Q

Mechanism

Doxazosin

Selective for?

A

Mechanism:

Block alpha-adrenoceptor mediated effects by direct competition

Q

Action

Doxazosin

Selective for?

A

Action:

Increased sympathetic drive (indirect - reflex)
Vasodilation
Decreased BP

Q

Side Effects (+ special features)

Doxazosin

Selective for?

A

Side Effects & Special Features:

Nasal stuffiness (due to vasodilation)
Reflex tachycardia
Postural hypotension
Sodium & water retention
Miosis (pupillary constriction)

Q

Class

Tamsulosin

Selective for?

A

Class:

alpha-adrenoceptor antagonist (alpha1 selective)

Q

Uses (treatments)

Tamsulosin

Selective for?

A

Uses:

Decrease BP
Decrease urinary retention
Allow kidney stone passage
Anti-hypertensive
Treatment of phaeochromocytoma (to decrease BP)
Reverse of dental local anaesthesia

Q

Mechanism

Tamsulosin

Selective for?

A

Mechanism:

Block alpha-adrenoceptor mediated effects by direct competition

Q

Action

Tamsulosin

Selective for?

A

Action:

Increased sympathetic drive (indirect - reflex)
Vasodilation
Decreased BP

Q

Side Effects (+ special features)

Tamsulosin

Selective for?

A

Side Effects & Special Features:

Nasal stuffiness (due to vasodilation)
Reflex tachycardia
Postural hypotension
Sodium & water retention
Miosis (pupillary constriction)

Q

Class

Propranolol

Selective for?

A

Class:

beta-adrenoceptor antagonist (non-selective)

Q

Uses (treatments)

Propranolol

Selective for?

A

Uses:

Treatment of angina
Hypertension
Heart failure
Glaucoma
Atrial dysrhthmias
For Haemodynamically stable patients –> helps with anxiety & migraines (5-HTr action)
Treats thyrotoxicosis

Q

Mechanism

Propranolol

Selective for?

A

Mechanism:

Block beta-adrenoceptor mediated effects by direct competition
Activation of baroreceptor reflex

Q

Action

Propranolol

Selective for?

A

Action:

Decreased cardiac output
Decreased sympathetic activity
Decreased BP
Vasoconstriction
Inhibit renin (beta 1 mediated)

Q

Side Effects (+ special features)

Propranolol

Selective for?

A

Side Effects & Special Features:

Bradycardia
Cold extremities (alpha-adrenoceptor baroreceptor reflex –> causes vasoconstriction)
Bronchospasm (contraindicated in asthmatics)
Baroreceptor resetting
Diabetics Beta-cell inhibition (insulin releasing cell)
Increase of preload –> increasing O2 demand of heart

Q

Class

Atenolol

Selective for?

A

Class:

Beta-adrenoceptor antagonist (beta 1 selective)

Q

Uses (treatments)

Atenolol

Selective for?

A

Uses:

Does not cross BBB (blood brain barrier)
Treatment of angina
Hypertension
Heart failure
Glaucoma
Atrial dysrhthmias
For Haemodynamically stable patients –> helps with anxiety & migraines (5-HTr action)
Treats thyrotoxicosis

Q

Mechanism

Atenolol

Selective for?

A

Mechanism:

Block beta-adrenoceptor mediated effects by direct competition
Activation of baroreceptor reflex

Q

Action

Atenolol

Selective for?

A

Action:

Decreased cardiac output
Decreased sympathetic activity
Decreased BP
Vasoconstriction
Inhibit renin (beta 1 mediated)

Q

Side Effects (+ special features)

Atenolol

Selective for?

A

Side Effects & Special Features:

Bradycardia
Cold extremities (alpha-adrenoceptor baroreceptor reflex –> causes vasoconstriction)
Bronchospasm (contraindicated in asthmatics)
Baroreceptor resetting
Diabetics Beta-cell inhibition (insulin releasing cell)
Increase of preload –> increasing O2 demand of heart

Q

Class

Carvedilol

Selective for?

A

Class:

Beta-adrenoceptor antagonist (non-selective)

Q

Uses (treatments)

Carvedilol

Selective for?

A

Uses:

Treatment of angina
Hypertension
Heart failure
Glaucoma
Atrial dysrhthmias
For Haemodynamically stable patients –> helps with anxiety & migraines (5-HTr action)
Treats thyrotoxicosis

Q

Mechanism

Carvedilol

Selective for?

A

Mechanism:

Block beta-adrenoceptor mediated effects by direct competition
Activation of baroreceptor reflex

Q

Action

Carvedilol

Selective for?

A

Action:

Decreased cardiac output
Decreased sympathetic activity
Decreased BP
Vasoconstriction
Inhibit renin (beta 1 mediated)

Q

Side Effects (+ special features)

Carvedilol

Selective for?

A

Side Effects & Special Features:

Bradycardia
Cold extremities (alpha-adrenoceptor baroreceptor reflex –> causes vasoconstriction)
Bronchospasm (contraindicated in asthmatics)
Baroreceptor resetting
Diabetics Beta-cell inhibition (insulin releasing cell)
Increase of preload –> increasing O2 demand of heart

Q

Class

Timolol

Selective for?

(No data - generic guessing)

A

Class:

Beta-adrenoceptor antagonist

Q

Uses (treatments)

Timolol

Selective for?

(No data - generic guessing)

A

Uses:

Treatment of angina
Hypertension
Heart failure
Glaucoma
Atrial dysrhthmias
For Haemodynamically stable patients –> helps with anxiety & migraines (5-HTr action)
Treats thyrotoxicosis

Q

Mechanism

Timolol

Selective for?

(No data - generic guessing)

A

Mechanism:

Block beta-adrenoceptor mediated effects by direct competition
Activation of baroreceptor reflex

Q

Action

Timolol

Selective for?

(No data - generic guessing)

A

Action:

Decreased cardiac output
Decreased sympathetic activity
Decreased BP
Vasoconstriction
Inhibit renin (beta 1 mediated)

Q

Side Effects (+ special features)

Timolol

Selective for?

(No data - generic guessing)

A

Side Effects & Special Features:

Bradycardia
Cold extremities (alpha-adrenoceptor baroreceptor reflex –> causes vasoconstriction)
Bronchospasm (contraindicated in asthmatics)
Baroreceptor resetting
Diabetics Beta-cell inhibition (insulin releasing cell)
Increase of preload –> increasing O2 demand of heart

Q

Class

Bisoprolol

Selective for?

NB: Drugs are never 100% truly selective (rarely)

A

Class:

Beta-adrenoceptor antagonist (beta 1 selective - cardioselective)

Q

Uses (treatments)

Bisoprolol

Selective for?

NB: Drugs are never 100% truly selective (rarely)

A

Uses:

Treatment of angina
Hypertension
Heart failure
Glaucoma
Atrial dysrhthmias
For Haemodynamically stable patients –> helps with anxiety & migraines (5-HTr action)
Treats thyrotoxicosis

Q

Mechanism

Bisoprolol

Selective for?

NB: Drugs are never 100% truly selective (rarely)

A

Mechanism:

Block beta-adrenoceptor mediated effects by direct competition
Activation of baroreceptor reflex

Q

Action

Bisoprolol

Selective for?

NB: Drugs are never 100% truly selective (rarely)

A

Action:

Decreased cardiac output
Decreased sympathetic activity
Decreased BP
Vasoconstriction
Inhibit renin (beta 1 mediated)

Q

Side Effects (+ special features)

Bisoprolol

Selective for?

NB: Drugs are never 100% truly selective (rarely)

A

Side Effects & Special Features:

Bradycardia
Cold extremities (alpha-adrenoceptor baroreceptor reflex –> causes vasoconstriction)
Bronchospasm (contraindicated in asthmatics)
Baroreceptor resetting
Diabetics Beta-cell inhibition (insulin releasing cell)
Increase of preload –> increasing O2 demand of heart

Q

Class

Dipivephrine

Selective for?

A

Class:

Pro-drug of adrenaline (adrenoceptor agonist - alpha effect) - alpha 2 selective

Q

Uses (treatments)

Dipivephrine

Selective for?

A

Uses:

Less potent than NA (but clinically used unlike NA)
Anaphylactic shock (epipens)
Cardiac arrest
Prolong action of local anaesthetics

Q

Mechanism

Dipivephrine

Selective for?

A

Mechanism:

alpha & beta action
Alpha1 –> phospholipase C activation –> IP3 & DAG formation –> increase in calcium release
Alpha2 –> inhibit adenylate cyclase –> decrease cAMP –> decrease Protein Kinase A (PKA)

Q

Action

Dipivephrine

Selective for?

A

Action:

alpha1 –> smooth muscle contraction, vasoconstriction, decrease GI motility, promote glycogenolysis
alpha2 –> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

Q

Side Effects (+ special features)

Dipivephrine

Selective for?

A

Side Effects & Special Features:

Hypertension
Reflex bradycardia
Vasoconstriction (activation of alpha-receptors)
High Dose given –> to overcome smooth muscle vessel vasodilation (beta 2 induced)
Activates alpha receptor to cause vasoconstriction

Q

Class

Tyramine

Selective for?

A

Class:

Indirectly acting sympathomimetics

Q

Uses (treatments)

Tyramine

Selective for?

A

Uses:

Treatment of Hypertension
Treatment of Angina
Treatment of Glaucoma

Q

Mechanism

Tyramine

Selective for?

A

Mechanism:

Displaces NA from vesicles taken up from synapse via VMAT (transporter) –> exchanged by NA
No exocytosis
NA diffuses out

Q

Action

Tyramine

Selective for?

A

Action:

Decreased heart rate
Decreased cardiac output
Reduced sympathetic drive to the heart
Decreased production of aqueous humour

Q

Side Effects (+ special features)

Tyramine

Selective for?

A

Side Effects & Special Features:

Bronchoconstriction (contraindicated in asthmatics)
Bradycardia
Cardiac failure
Tyramine –> metabolised by MAO in intestines
MAO Inhibiiton –> tyramine absorbed –> vasoconstriction at post-junctional alpha-receptor

Q

Class

Ephedrine

Selective for?

A

Class:

Indirectly acting sympathomimetics

Q

Uses (treatments)

Ephedrine

Selective for?

A

Uses:

Treatment of Hypertension
Treatment of Angina
Treatment of Glaucoma

Q

Mechanism

Ephedrine

Selective for?

A

Mechanism:

Displaces NA from vesicles taken up from synapse via VMAT (transporter) –> exchanged by NA
No exocytosis (vesicular transport)
NA diffuses out

Q

Action

Ephedrine

Selective for?

A

Action:

Decreased heart rate
Decreased cardiac output
Reduced sympathetic drive to the heart
Decreased production of aqueous humour

Q

Side Effects (+ special features)

Ephedrine

Selective for?

A

Side Effects & Special Features:

Bronchoconstriction (contraindicated in asthmatics)
Bradycardia
Cardiac failure

Q

Class

Amphetamine

Selective for?

A

Class:

Indirectly acting sympathomimetics

Q

Uses (treatments)

Amphetamine

Selective for?

A

Uses:

Treatment of Hypertension
Treatment of Angina
Treatment of Glaucoma

Q

Mechanism

Amphetamine

Selective for?

A

Mechanism:

Displaces NA from vesicles taken up from synapse via VMAT (transporter) –> exchanged by NA
No exocytosis (vesicular transport)
NA diffuses out

Q

Action

Amphetamine

Selective for?

A

Action:

Decreased heart rate
Decreased cardiac output
Reduced sympathetic drive to the heart
Decreased production of aqueous humour

Q

Side Effects (+ special features)

Amphetamine

Selective for?

A

Side Effects & Special Features:

Bronchoconstriction (contraindicated in asthmatics)
Bradycardia
Cardiac failure

Q

Class

Ergometrine

Selective for?

A

Class:

Ergot alkaloids

Q

Uses (treatments)

Ergometrine

Selective for?

A

Uses:

Migraines
Anti-hypertensives
Treatment of phaeochromocytomas (to reduce BP)
Reversal of dental local anaesthesia

Q

Mechanism

Ergometrine

Selective for?

A

Mechanism:

Block alpha-adrenoceptor mediated effected by direct competition

Q

Action

Ergometrine

Selective for?

A

Action:

Increased sympathetic drive (indirect)
Vasodilation
Decreased BP

Q

Side Effects (+ special features)

Ergometrine

Selective for?

A

Side Effects & Special Features:

Nasal stuffiness
Reflex tachycardia
Postural hypotension
Sodium & water retention
Miosis (pupillary constriction)

Q

Class

Bromocriptine

Selective for?

A

Class:

Ergot alkaloids

Q

Uses (treatments)

Bromocriptine

Selective for?

A

Uses:

Postpartum haemorrhage
Dementia (cerebral vasodilator)
Anti-hypertensives
Treatment of phaeochromocytomas (to reduce BP)
Reversal of dental local anaesthesia

Q

Mechanism

Bromocriptine

Selective for?

A

Mechanism:

Block alpha-adrenoceptor mediated effected by direct competition

Q

Action

Bromocriptine

Selective for?

A

Action:

Increased sympathetic drive (indirect)
Vasodilation
Decreased BP

Q

Side Effects (+ special features)

Bromocriptine

Selective for?

A

Side Effects & Special Features:

Nasal stuffiness
Reflex tachycardia
Postural hypotension
Sodium & water retention
Miosis (pupillary constriction)

Q

Class

Reserpine

A

Class:

Adrenergic neurone drugs (VMAT Inhibitors)

Q

Uses (treatments)

Reserpine

A

Uses:

Pyschosis
Shuts down ANS
Treatment of hyperkinetic disorders (e.g. huntington)

Q

Mechanism

Reserpine

A

Mechanism:

Inhibits NA storage in veiscles by VMAT (vesicular monoamine transporter)
Irreversible blockage
Monoamines leak from the cytoplasm OR inactivated by MAO

Q

Action

Reserpine

A

Action:

Shuts down ANS

Q

Side Effects (+ special features)

Reserpine

A

Side Effects & Special Features:

Causes depression in 15% of patients
Inhibits VMAT –> promoting early degradation of monoamines
Effects reversed with MAO Inhibitors (MAOI)
MDMA inhibits MAO/VMAT
(Displacement of 5HT –> hypotension, loss of consciousness, seizures, rhabdomyolysis, intravascular disseminated coagulation

Q

Class

Guanethidine

Selective for?

A

Class:

Indirectly acting sympathomimetics (adrenergic neurone drug)

Q

Uses (treatments)

Guanethidine

Selective for?

A

Uses:

Na+ Channel Blocker too –> Local Anaesthetic
Treatment of Hypertension
Treatment of Angina
Treatment of Glaucoma

Q

Mechanism

Guanethidine

Selective for?

A

Mechanism:

Inhibits NA release
Sodium channel blocker

Q

Action

Guanethidine

Selective for?

A

Action:

Decreased heart rate
Decreased cardiac output
Reduced sympathetic drive to the heart
Decreased production of aqueous humour

Q

Side Effects (+ special features)

Guanethidine

Selective for?

A

Side Effects & Special Features:

Bronchoconstriction (contraindicated in asthmatics)
Bradycardia
Cardiac failure

Q

Class

Cocaine

Selective for?

A

Class:

Noradrenaline-Uptake 1 Inhibitors

Q

Uses (treatments)

Cocaine

Selective for?

A

Uses:

Treatment of Hypertension
Treatment of Angina
Treatment of Glaucoma

Q

Mechanism

Cocaine

Selective for?

A

Mechanism:

Inhibits NA re-uptake-1 (pre-synaptically)

Q

Action

Cocaine

Selective for?

A

Action:

Decreased heart rate
Decreased cardiac output
Reduced sympathetic drive to the heart
Decreased production of aqueous humour

Q

Side Effects (+ special features)

Cocaine

Selective for?

A

Side Effects & Special Features:

Bronchoconstriction (contraindicated in asthmatics)
Bradycardia
Cardiac failure

Q

Class

Desmethylimipramine (desipramine)

Selective for?

A

Class:

Noradrenaline-Uptake 1 Inhibitors (Tricyclic Antidepressant)

Q

Uses (treatments)

Desmethylimipramine (desipramine)

Selective for?

A

Uses:

Treatment of Hypertension
Treatment of Angina
Treatment of Glaucoma

Q

Mechanism

Desmethylimipramine (desipramine)

Selective for?

A

Mechanism:

Inhibits NA re-uptake-1 (pre-synaptically)

Q

Action

Desmethylimipramine (desipramine)

Selective for?

A

Action:

Decreased heart rate
Decreased cardiac output
Reduced sympathetic drive to the heart
Decreased production of aqueous humour

Q

Side Effects (+ special features)

Desmethylimipramine (desipramine)

Selective for?

A

Side Effects & Special Features:

Bronchoconstriction (contraindicated in asthmatics)
Bradycardia
Cardiac failure

Q

Name 2 B-adrenoceptor antagoinists that have Intinisic sympathomimetic activity (ISA)

A

Pindolol and oxprenolol

Q

What does intrinisc sympathomimetic activity (ISA) mean?

A

Means that they are antagoniists but can also have sympathetic effects so they are agonist and antagonists! aka partial agonists

Q

Name a lipid soluble b blocker and a water soluble b blocker

A

lipid soluble==> propranolol

water soluble ==> atenolol

Q

Name a B1 antagonist but is also a B3 agonist

A

Nebivolol

Q

What do B3 receptors do?

A

They are found in endothelium and when stimulated they relase NO which causes vasodilation

Q

function of carvedilol and labetatol

A

They have combined a/B1 adrenoceptor antagonist propeties so they slow heart rate (by blocking B receptors) but also decrease peripheral resistance by blocking alpha adrenoceptors

Q

A

Q

What drug can be used to treat phaechromocytoma by blocking the rate determining step of conerting tyrosine into L-DOPA

A

alpha-methyltyrosine!