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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# Side Effects (+ special features) Phenylephrine Alpha or beta effect? (predominantely)

**Side Effects & Special Features:** * Hypertension * Reflex bradycardia * Vasoconstriction (activation of alpha-receptors)

# Class Clonidine Specific target?

**Class:** Adrenoceptor Agonist (alpha2 target)

# Uses (treatments) Clonidine Specific target?

**Uses:** * **Imidazoline receptor agonist (CNS)** --\> anti-hypertensive, anxiolytic, attention deficit, hyperactivity, withdrawal

# Mechanism Clonidine Specific target?

**Mechanism:** * **alpha2** --\> inhibit adenylate cyclase --\> decrease cAMP --\> decrease Protein Kinase A (PKA)

# Action Clonidine Specific target?

**Action:** * **alpha2** --\> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

# Side Effects (+ special features) Clonidine Specific target?

**Side Effects & Special Features:** * Hypertension (probably not) * Reflex bradycardia (probably not) * Vasoconstriction (activation of alpha-receptors)

# Class Brimonidine

**Class:** Adrenoceptor Agonist (alpha2)

# Uses (treatments) Brimonidine

**Uses:** * **Treatment of _open_ angle glaucoma**

# Mechanism Brimonidine

**Mechanism:** * **alpha2** --\> inhibit adenylate cyclase --\> decrease cAMP --\> decrease Protein Kinase A (PKA)

# Action Brimonidine

**Action:** * **alpha2** --\> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

# Side Effects (+ special features) Brimonidine

**Side Effects & Special Features:** * Hypertension (probably not) * Reflex bradycardia (probably not) * Vasoconstriction (activation of alpha-receptors)

# Class alpha-methylnoradrenaline

Central-acting alpha 2 agonists

# Class Salbutamol Specific effect on?

**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

# Uses (treatments) Salbutamol Specific effect on?

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

# Mechanism Salbutamol Specific effect on?

**Mechanism:** * Increased cAMP * **Activation of Protein Kinase A (PKA)** --\> leads to **protein** **phosphorylation**

# Action Salbutamol Specific effect on?

**Action:** * **beta2** --\> smooth muscle relaxation (bronchodilation), smooth muscle vasodilation

# Side Effects (+ special features) Salbutamol Specific effect on?

**Side Effects & Special Features:** * Hypokalaemia * Tremor * Hypotension * Reflex tachycardia

# Class Dobutamine Specific effect on?

**Class:** Adrenoceptor Agonist (beta 1 receptor effect)

# Uses (treatments) Dobutamine Specific effect on?

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

# Mechanism Dobutamine Specific effect on?

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

# Action Dobutamine Specific effect on?

**Action:** * **beta1** --\> Increase heart rate & contractile force, vasodilation, renin release, inhibition of histamine, increased glycogenolysis & lipolysis

# Side Effects (+ special features) Dobutamine Specific effect on?

**Side Effects & Special Features:** * Hypokalaemia * Tremor * Hypotension * Reflex tachycardia

# Class Phentolamine

**Class:** alpha-adrenoceptor antagonist

# Uses (treatments) Phentolamine

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

# Mechanism Phentolamine

**Mechanism:** * Block alpha-adrenoceptor mediated effects by direct competition

# Action Phentolamine

**Action:** * Increased sympathetic drive (indirect - reflex) * Vasodilation * Decreased BP

# Side Effects (+ special features) Phentolamine

**Side Effects & Special Features:** * Nasal stuffiness (due to vasodilation) * Reflex tachycardia * Postural hypotension * Sodium & water retention * Miosis (pupillary constriction)

# Class Phenoxybenzamine

**Class:** alpha-adrenoceptor antagonist

# Uses (treatments) Phenoxybenzamine

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

# Mechanism Phenoxybenzamine

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

# Action Phenoxybenzamine

**Action:** * Increased sympathetic drive (indirect - reflex) * Vasodilation * Decreased BP

# Side Effects (+ special features) Phenoxybenzamine

**Side Effects & Special Features:** * Nasal stuffiness (due to vasodilation) * Reflex tachycardia * Postural hypotension * Sodium & water retention * Miosis (pupillary constriction)

# Class Prazosin Selective for?

**Class:** alpha-adrenoceptor antagonist (alpha1 selective)

# Uses (treatments) Prazosin Selective for?

**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

# Mechanism Prazosin Selective for?

**Mechanism:** * Block alpha-adrenoceptor mediated effects by direct competition

# Action Prazosin Selective for?

**Action:** * Increased sympathetic drive (indirect - reflex) * Vasodilation * Decreased BP

# Side Effects (+ special features) Prazosin Selective for?

**Side Effects & Special Features:** * Nasal stuffiness (due to vasodilation) * Reflex tachycardia * Postural hypotension * Sodium & water retention * Miosis (pupillary constriction)

# Class Doxazosin Selective for?

**Class:** alpha-adrenoceptor antagonist (alpha1 selective)

# Uses (treatments) Doxazosin Selective for?

**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

# Mechanism Doxazosin Selective for?

**Mechanism:** * Block alpha-adrenoceptor mediated effects by direct competition

# Action Doxazosin Selective for?

**Action:** * Increased sympathetic drive (indirect - reflex) * Vasodilation * Decreased BP

# Side Effects (+ special features) Doxazosin Selective for?

**Side Effects & Special Features:** * Nasal stuffiness (due to vasodilation) * Reflex tachycardia * Postural hypotension * Sodium & water retention * Miosis (pupillary constriction)

# Class Tamsulosin Selective for?

**Class:** alpha-adrenoceptor antagonist (alpha1 selective)

# Uses (treatments) Tamsulosin Selective for?

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

# Mechanism Tamsulosin Selective for?

**Mechanism:** * Block alpha-adrenoceptor mediated effects by direct competition

# Action Tamsulosin Selective for?

**Action:** * Increased sympathetic drive (indirect - reflex) * Vasodilation * Decreased BP

# Side Effects (+ special features) Tamsulosin Selective for?

**Side Effects & Special Features:** * Nasal stuffiness (due to vasodilation) * Reflex tachycardia * Postural hypotension * Sodium & water retention * Miosis (pupillary constriction)

# Class Propranolol Selective for?

**Class:** beta-adrenoceptor antagonist (non-selective)

# Uses (treatments) Propranolol Selective for?

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

# Mechanism Propranolol Selective for?

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

# Action Propranolol Selective for?

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

# Side Effects (+ special features) Propranolol Selective for?

**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

# Class Atenolol Selective for?

**Class:** Beta-adrenoceptor antagonist (beta 1 selective)

# Uses (treatments) Atenolol Selective for?

**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

# Mechanism Atenolol Selective for?

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

# Action Atenolol Selective for?

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

# Side Effects (+ special features) Atenolol Selective for?

**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

# Class Carvedilol Selective for?

**Class:** Beta-adrenoceptor antagonist (non-selective)

# Uses (treatments) Carvedilol Selective for?

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

# Mechanism Carvedilol Selective for?

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

# Action Carvedilol Selective for?

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

# Side Effects (+ special features) Carvedilol Selective for?

**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

# Class Timolol Selective for? (No data - generic guessing)

**Class:** Beta-adrenoceptor antagonist

# Uses (treatments) Timolol Selective for? (No data - generic guessing)

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

# Mechanism Timolol Selective for? (No data - generic guessing)

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

# Action Timolol Selective for? (No data - generic guessing)

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

# Side Effects (+ special features) Timolol Selective for? (No data - generic guessing)

**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

# Class Bisoprolol Selective for? NB: Drugs are never 100% truly selective (rarely)

**Class:** Beta-adrenoceptor antagonist (beta 1 selective - cardioselective)

# Uses (treatments) Bisoprolol Selective for? NB: Drugs are never 100% truly selective (rarely)

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

# Mechanism Bisoprolol Selective for? NB: Drugs are never 100% truly selective (rarely)

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

# Action Bisoprolol Selective for? NB: Drugs are never 100% truly selective (rarely)

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

# Side Effects (+ special features) Bisoprolol Selective for? NB: Drugs are never 100% truly selective (rarely)

**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

# Class Dipivephrine Selective for?

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

# Uses (treatments) Dipivephrine Selective for?

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

# Mechanism Dipivephrine Selective for?

**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)

# Action Dipivephrine Selective for?

**Action:** * alpha1 --\> smooth muscle contraction, vasoconstriction, decrease GI motility, promote glycogenolysis * alpha2 --\> inhibit noradrenaline & decrease lipolysis, decrease aqueous humour production

# Side Effects (+ special features) Dipivephrine Selective for?

**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**

# Class Tyramine Selective for?

**Class:** Indirectly acting sympathomimetics

# Uses (treatments) Tyramine Selective for?

**Uses:** * Treatment of Hypertension * Treatment of Angina * Treatment of Glaucoma

# Mechanism Tyramine Selective for?

**Mechanism:** * Displaces NA from vesicles taken up from synapse via VMAT (transporter) --\> exchanged by NA * No exocytosis * NA diffuses out

# Action Tyramine Selective for?

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

# Side Effects (+ special features) Tyramine Selective for?

**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

# Class Ephedrine Selective for?

**Class:** Indirectly acting sympathomimetics

# Uses (treatments) Ephedrine Selective for?

**Uses:** * Treatment of Hypertension * Treatment of Angina * Treatment of Glaucoma

# Mechanism Ephedrine Selective for?

**Mechanism:** * Displaces NA from vesicles taken up from synapse via VMAT (transporter) --\> exchanged by NA * No exocytosis (vesicular transport) * NA diffuses out

# Action Ephedrine Selective for?

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

# Side Effects (+ special features) Ephedrine Selective for?

**Side Effects & Special Features:** * Bronchoconstriction (contraindicated in asthmatics) * Bradycardia * Cardiac failure

# Class Amphetamine Selective for?

**Class:** Indirectly acting sympathomimetics

# Uses (treatments) Amphetamine Selective for?

**Uses:** * Treatment of Hypertension * Treatment of Angina * Treatment of Glaucoma

# Mechanism Amphetamine Selective for?

**Mechanism:** * Displaces NA from vesicles taken up from synapse via VMAT (transporter) --\> exchanged by NA * No exocytosis (vesicular transport) * NA diffuses out

# Action Amphetamine Selective for?

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

# Side Effects (+ special features) Amphetamine Selective for?

**Side Effects & Special Features:** * Bronchoconstriction (contraindicated in asthmatics) * Bradycardia * Cardiac failure

# Class Ergometrine Selective for?

**Class:** Ergot alkaloids

# Uses (treatments) Ergometrine Selective for?

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

# Mechanism Ergometrine Selective for?

**Mechanism:** * Block alpha-adrenoceptor mediated effected by direct competition

# Action Ergometrine Selective for?

**Action:** * Increased sympathetic drive (indirect) * Vasodilation * Decreased BP

# Side Effects (+ special features) Ergometrine Selective for?

**Side Effects & Special Features:** * Nasal stuffiness * Reflex tachycardia * Postural hypotension * Sodium & water retention * Miosis (pupillary constriction)

# Class Bromocriptine Selective for?

**Class:** Ergot alkaloids

# Uses (treatments) Bromocriptine Selective for?

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

# Mechanism Bromocriptine Selective for?

**Mechanism:** * Block alpha-adrenoceptor mediated effected by direct competition

# Action Bromocriptine Selective for?

**Action:** * Increased sympathetic drive (indirect) * Vasodilation * Decreased BP

# Side Effects (+ special features) Bromocriptine Selective for?

**Side Effects & Special Features:** * Nasal stuffiness * Reflex tachycardia * Postural hypotension * Sodium & water retention * Miosis (pupillary constriction)

# Class Reserpine

**Class:** Adrenergic neurone drugs (VMAT Inhibitors)

# Uses (treatments) Reserpine

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

# Mechanism Reserpine

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

# Action Reserpine

**Action:** * Shuts down ANS

# Side Effects (+ special features) Reserpine

**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

# Class Guanethidine Selective for?

**Class:** Indirectly acting sympathomimetics (adrenergic neurone drug)

# Uses (treatments) Guanethidine Selective for?

**Uses:** * **Na+ Channel Blocker too --\> Local Anaesthetic** * Treatment of Hypertension * Treatment of Angina * Treatment of Glaucoma

# Mechanism Guanethidine Selective for?

**Mechanism:** * Inhibits NA release * Sodium channel blocker

# Action Guanethidine Selective for?

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

# Side Effects (+ special features) Guanethidine Selective for?

**Side Effects & Special Features:** * Bronchoconstriction (contraindicated in asthmatics) * Bradycardia * Cardiac failure

# Class Cocaine Selective for?

**Class:** Noradrenaline-Uptake 1 Inhibitors

# Uses (treatments) Cocaine Selective for?

**Uses:** * Treatment of Hypertension * Treatment of Angina * Treatment of Glaucoma

# Mechanism Cocaine Selective for?

**Mechanism:** * Inhibits NA re-uptake-1 (pre-synaptically)

# Action Cocaine Selective for?

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

# Side Effects (+ special features) Cocaine Selective for?

**Side Effects & Special Features:** * Bronchoconstriction (contraindicated in asthmatics) * Bradycardia * Cardiac failure

# Class Desmethylimipramine (desipramine) Selective for?

**Class:** Noradrenaline-Uptake 1 Inhibitors (Tricyclic Antidepressant)

# Uses (treatments) Desmethylimipramine (desipramine) Selective for?

**Uses:** * Treatment of Hypertension * Treatment of Angina * Treatment of Glaucoma

# Mechanism Desmethylimipramine (desipramine) Selective for?

**Mechanism:** * Inhibits NA re-uptake-1 (pre-synaptically)

# Action Desmethylimipramine (desipramine) Selective for?

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

# Side Effects (+ special features) Desmethylimipramine (desipramine) Selective for?

**Side Effects & Special Features:** * Bronchoconstriction (contraindicated in asthmatics) * Bradycardia * Cardiac failure

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

Pindolol and oxprenolol

What does intrinisc sympathomimetic activity (ISA) mean?

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

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

lipid soluble==\> propranolol water soluble ==\> atenolol

Name a B1 antagonist but is also a B3 agonist

**Nebivolol**

What do B3 receptors do?

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

function of **carvedilol** and **labetatol**

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

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

alpha-methyltyrosine!