UNIT- V (PHARMACOLOGY FOR NURSES) 3rd SEMESTER

Classification of nervous system

NERVOUS SYSTEM

CENTRAL NERVOUS PERIPHERAL NERVOUS

SYSTEM SYSTEM

AUTONOMIC NERVOUS SOMATIC NERVOUS

SYSTEM SYSTEM

PARASYMPATHETIC
SYMPATHETIC SYSTEM
SYSTEM

SYMPATHETIC NERVOUS SYSTEM

• Efferent division has two neurons.

• The junction between neurons is called
ganglia.
• Preganglionic neuron releases – Ach
• Postganglionic neuron releases - NA

• Precursor of NA – tyrosine
• Tyrosine → DOPA → Dopamine → NA.
• NA metabolized by MAO & COMT.
• NA acts on adrenergic receptors to
produce action

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Receptor subtype and action

RECEPTOR LOCATION RESPONSE

TYPE
ꞵ1 • Heart • ↑se HR, FoC & Conduction velocity
• Kidney • Renin release
ꞵ2 • Smooth muscle (vascular, • Relaxation
bronchial, gut,
genitourinary) • glycogenolysis
• liver
ꞵ3 • Adipose tissue • lipolysis

α1 • Smooth muscle • contraction

• Radial muscles of iris
α2 • Beta cells • ↓se insulin release
• Nerve terminal • ↓se neurotransmitter release

Therapeutic Classification

▪ Vasopressors : Noradrenaline, Phenylephrine, Methoxamine,

Dopamine,

▪ Cardiac stimulants : Adrenaline, Dobutamine, Isoprenaline

▪ Bronchodilator : Isoprenaline, Salbutamol(Albuterol), Terbutaline,

Salmeterol, formoterol, Bambuterol

▪ Nasal decongestants : Phenylephrine, Xylometazoline, Oxymetazoline,

Naphazoline, Pseudoephedrine,

▪ CNS stimulants : Amphetamine, Methamphetamine, Dexamphetamine

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▪ Anorectics : Fenfluramine, Sibutramine, Dexfenfluramine

▪ Uterine relaxant : Ritodrine, Isoxsuprine, Salbutamol, Terbutaline

Adrenaline Vs Noradrenaline

Compare and contrast adrenaline and noradrenaline

Feature Adrenaline Noradrenaline
Chemistry Catecholamine Catecholamine
On adrenergic receptors Agonist Agonist
Receptor selectivity Both α & ꞵ Predominantly α
Dale’s vasomotor reversal Yes No
Clinical uses Many Rarely used
Major indication • Anaphylactic shock Rarely used in hypertension
• Cardiac arrest

Uses of Adrenaline

1. Anaphylactic shock: Adrenaline is the drug of choice (0.3-0.5 mL of 1:1000

solution). It promptly reverses hypotension, laryngeal edema and bronchospasm and
is life- saving in anaphylactic shock.

• IM route is preferred as absorption by SC route is not reliable in shock

2. Cardiac arrest: Sudden cardiac arrest due to drowning, electrocution, etc., are treated
with intracardiac adrenaline

3. Control of hemorrhage: Cotton or gauze soaked in adrenaline- 1:10,000 to 1:20,000

concentration is used as a topical hemostatic to control bleeding. Bleeding stops due to
vasoconstriction. Adrenaline packs are used to control bleeding after tooth extraction
and in epistaxis.

4. With local anesthetics : Injected with LA, adrenaline produces vasoconstriction

and reduces the rate of absorption of the LA → prolongs the action of the LA & reduces
systemic toxicity

5. Bronchial asthma: Adrenaline produces bronchodilation.

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6. Glaucoma: Adrenaline ↓se IOP and can be used in glaucoma. Dipivefrin is a prodrug
which gets converted to adrenaline in the eye by the action of corneal esterases.
Dipivefrin has good penetrability due to high lipid solubility and it is used in glaucoma.

ALPHA 2 AGONISTS

▪ Clonidine, apraclonidine and brimonidine are selective alpha 2 agonists.

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▪ Clonidine is used in hypertension.

▪ Apraclonidine and brimonidine are used in glaucoma as they lower intraocular
pressure.

SELECTIVE ẞ₂ STIMULANTS

Salbutamol, Terbutaline, Salmeterol, Perbuterol, Bitolterol, Fenoterol, Formoterol.

• These are smooth muscle relaxants

• Produce bronchodilatation, vasodilation and uterine relaxation without
significant cardiac stimulation.
• Salbutamol and other ẞ₂ stimulants can be given by inhalation.

Side effects
• muscle tremors, palpitation and arrhythmias.

Uses
• Bronchial asthma
• As uterine relaxants to delay premature labor.
• Isoxsuprine is a selective ẞ2 receptor stimulant used as uterine relaxant in
premature labor, threatened abortion and dysmenorrhea
ANTIADRENERGIC DRUGS

ALPHA ADRENERGIC BLOCKERS

ALPHA BLOCKERS

NON-SELECTIVE SELECTIVE

COMPETITIVE α1 BLOCKER α2 BLOCKER

Prazosin, yohimbine
NONCOMPETITIVE ergotamine,
phenoxybenzamine phentolamine, Terazosin,
tolazoline, Doxazosin,
chlorpromazine Alfuzosin,
Tamsulosin

α1 BLOCKER

PRAZOSIN, TERAZOSIN, DOXAZOSIN

▪ Used in hypertension

▪ increase HDL & decrease LDL

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First dose effect-

Tamsulosin (α1 A blocker), Alfuzosin

▪ Indicated for the treatment of benign prostatic hypertrophy or BPH

Due to relaxation of smooth muscle in the neck of urinary bladder, urinary flow is
improved by these drugs

Uses
1. Hypertension: Selective a₁-blockers, such as prazosin are used in the treatment of
hypertension.
• Phenoxybenzamine or phentolamine can be used in hypertensive crisis
2. Benign prostatic hypertrophy (BPH): Blockade of α1receptors in the bladder,
prostate and urethra reduce resistance to urine outflow.
3. Pheochromocytoma is an adrenal medullary tumor which secretes large amounts
of catecholamines resulting in hypertension. The tumor has to be removed
surgically. Phenoxybenzamine and phentolamine are used for the preoperative
management of the patient and during the operation. Inoperable cases are put on
long-term treatment with phenoxybenzamine.
4. Congestive cardiac failure: Because of its vasodilator action, prazosin is useful in
CCF. But ACE inhibitors are preferred.
5. Peripheral vascular diseases, such as Raynaud's phenomenon may be benefited
by a-blockers which afford symptomatic relief.

BETA ADRENERGIC BLOCKERS

BETA BLOCKERS

ALPHA + BETA
NON SELECTIVE CARDIOSELECTIVE BLOCKER
propranolol, Timolol, Sotalol, Metoprolol, Atenolol, Acebutalol, Labetolol
Pindolol, Nadolol Celiprolol, Bisoprolol, Betaxolol, Carvedilol
Esmolol, Nebivolol

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Actions of beta blockers

HEART -
↓ HR, ↓
FoC, ↓ CO

LUNGS - EYE -
Bronchoco BETA
nstriction BLOCKERS ↓se IOP

LIVER - ↓se
glycogenolysis

Drug interaction

Propranolol + insulin

• When diabetics on insulin also receive propranolol;

• Beta-blockade masks tachycardia which is the first warning signal of hypoglycemia.
• Beta-blockade delays the recovery from hypoglycemia
• Solution: This may be avoided by using a ẞ₁ selective blocker.

Uses

1. Hypertension: B-blockers are useful in the treatment of mild to moderate

hypertension.

2. Angina pectoris: prophylaxis of exertional angina. → severity and frequency are

reduced. → reduce both cardiac work and O₂ demand.

3. Cardiac arrhythmias: B-blockers are useful in the treatment of both ventricular

and supraventricular arrhythmias. Sotalol has additional antiarrhythmic effects

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4. Myocardial infarction: B-blockers in acute MI may limit the size of the infarct.

5. Congestive cardiac failure: Sympathetic system is stimulated in CCF. →

Blocking the ẞ receptors → improve cardiac function & prevent cardiac
remodelling.

6. Obstructive cardiomyopathy: B-blockers are found to be beneficial.

7. Pheochromocytoma: Propranolol is given with alpha-blockers before surgery to

control hypertension

8. Thyrotoxicosis: Propranolol controls palpitation, tremors and affords

symptomatic relief in thyrotoxicosis; it is used as an adjuvant.

9. Glaucoma: Timolol is used topically in open angle glaucoma.

10. Prophylaxis of migraine: Propranolol reduces the frequency and severity of

migraine headache; used for prophylaxis.

11. Anxiety: Propranolol → Tremors, tachycardia and other symptoms of

sympathetic overactivity are alleviated.

12. Cirrhosis: ẞ-blockers may help by reducing the portal venous pressure.

13. Alcohol withdrawal: B-blockers help to overcome alcohol withdrawal symptoms

by reducing the central sympathetic overactivity.

14. Esophageal varices: In patients with bleeding varices, ẞ-blockers reduce

rebleeding.

CHOLINERGIC DRUGS

• Preganglionic neuron releases – Ach

• Postganglionic neuron releases - Ach

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• Ach metabolized by Cholinesterase.

• NA acts on Cholinergic receptors to
produce action.

Receptor subtypes and action

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CHOLINERGIC DRUGS – Direct acting

Choline esters Alkaloids

Acetyl choline Pilocarpine

Methacholine

Carbachol

Bethanechol

Actions of Acetylcholine

Organ Effect produced by cholinergic stimulation

Eye Miosis → ↑sed drainage of aqueous humor

Heart ↓se in HR, FoC, Conduction velocity

Blood vessels Dilation (mediated through EDRF - NO),

Lungs Bronchoconstriction
MUSCARINIC
GIT Increased motility

Relaxation of sphincters

Increased secretions

Urinary bladder Constriction of detrusor muscle and

relaxation of sphincters

Glands Stimulation
(exocrine)

NMJ Muscle contraction NICOTINIC

Ganglia stimulation

Uses

Bethanechol:

▪ used to stimulate the atonic bladder i.e., in postpartum or postoperative non-

obstructive urinary retention.
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▪ To treat neurogenic atony and megacolon.

Carbachol : Can be used as a miotic agent to treat glaucoma

Pilocarpine

▪ Glaucoma: it causes miosis and reduces IOP. Pilocarpine ocusert can deliver
pilocarpine constantly for 7 days.

▪ Pilocarpine is also used alternately with mydriatics, such as homatropine to break

the adhesions between the iris and the lens.

▪ It is used to counter dryness of mouth that is seen following radiation of head

and neck.

Cevimeline a derivative of acetylcholine directly stimulates the muscarinic receptors and

can be used to increase salivary secretions in Sjogren's syndrome and radiation-induced
xerostomia

Indirect acting cholinergic drugs

ANTICHOLINESTERASES

Reversible Irreversible

Carbamates Organophosphates Carbamates

Physostigmine Echothiophate Carbaryl

Neostigmine Malathion (SEVIN)
Pyridostigmine Sumithion Propoxur
Edrophonium Toxic nerve gases- (BAYGON)
Rivastigmine Tabun, Aldicarb
Donepezil Sarin, (TEMIK)
Galantamine

Physostigmine Vs Neostigmine

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Uses – reversible anticholinesterase

1. Myasthenia gravis:

• Reversible anticholinesterases- Treatment can be started with Neostigmine,

Pyridostigmine is an alternative which requires less frequent dosing.
• Immunosuppressants- Corticosteroids (Prednisolone), Azathioprine,
Cyclosporine: Inhibit the production of nicotinic receptor antibody
• Plasmapheresis (plasma exchange)- Removal of antibodies.

2. As a miotic: Physostigmine causes miosis, spasm of accommodation and a ↓ IOP. It is

used in:
• Glaucoma-can be used with pilocarpine for better effect.
• Alternately with a mydriatic to break adhesions between the iris and the lens.
• To reverse the effects of mydriatics.

3. Poisoning due to anticholinergic drugs: Physostigmine is used in atropine

poisoning and in toxicity due to other drugs with anticholinergic activity, such as
phenothiazines, tricyclic antidepressants and antihistamines. Because physostigmine
crosses the BBB, it reverses all the symptoms of atropine poisoning including CNS effects.

4. Curare poisoning: Skeletal muscle paralysis caused by curare can be antagonized by

AntiChEs. Though edrophonium has fast action, it is less effective than neostigmine.

5. Postoperative paralytic ileus and urinary retention: Neostigmine (subcutaneous)

may be useful.

6. Cobra bite: Cobra venom, a neurotoxin causes skeletal muscle paralysis. Specific
treatment is antivenom. Intravenous edrophonium prevents respiratory paralysis.

7. Alzheimer’s disease: Cerebroselective anti-ChEs, Rivastigmine, Donepezil and

Galantamine are commonly used.

Irreversible Anticholinesterase
▪ Organophosphorus (OP) compounds are powerful inhibitors of AChE enzyme;
binding with the enzyme is stable by covalent bonds.
▪ Effects are similar to that of cholinergic stimulation as ACh accumulates in the
tissues.
OP Poisoning

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Treatment

1. If poisoning is
• through skin → remove clothing + wash the skin with soap and water;
• by oral route → gastric lavage
2. Patient should be put in prone position to avoid aspiration of secretions.
3. Maintain BP and patent airway.
4. Drug of choice is atropine IV 2 mg every 10 minutes till pupil dilates.
5. Cholinesterase reactivators: Pradiloxime, obidoxime, diacetylmonoxime –
combine with cholinesterase organophosphate complex, release the binding and
set free AChE enzyme.

ANTI-CHOLINERGICS

Classification

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Uses - Atropine derivatives

Atropine Vs Scopolamine

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Contraindication
• Narrow angle glaucoma.
• Elderly patients.

PREVIOUS UNIVERSITY QUESTIONS

ESSAY

• Mention four anticholinergic drugs. Explain the uses of Atropine and its substitutes.
(2+5)

• Classify Beta blockers with suitable examples and write the uses and contra-
indications of propranolol. (3+4)

5 MARKS

• Anti cholinergic drugs

• Adrenaline
• Beta blockers*
• Uses of beta blockers*
• Uses and adverse effects of atropine and its substitutes
• Uses of atropine and its derivatives
• Nursing implication.
a. Management of organophosphate poisoning
• Treatment of organophosphorus poisoning*
• Uses of atropine and its derivatives
• Acetylcholine and adrenaline

4 MARKS

• Adrenergic drugs and their uses

• Differentiate between
o Adrenaline and noradrenaline*
o Atropine and scopolamine
o Propranolol and metoprolol
o Physostigmine and neostigmine
o Propranolol and metoprolol
o Cholinergics and anticholinergics

2 MARKS
• β blockers should be avoided in patients receiving insulin – Give reason.
• Adrenaline is used in anaphylaxis – Give reason
• Cholinomimetic drugs - define

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