Sympathetic System- Introduction, Definition, Classification, Receptor (with its types & location & action), neurotransmittor present in it.
[Classification, chemical name, chemical structure (of compounds with * mark), uses, stability and storage conditions, different types of formulation & their popular brand names of all the drug mentioned below]
A)Sympathomimetic Agents:
1. Direct Acting: Nor Epinephrine*, Epinephrine, Phenylephrine, Dopamine*, Terbutaline, Salbutamol (Albuterol), Naphazoline*, Tetrahydrozoline.
2. Indirect Acting Agents: Hydroxy Amphetamine, Pseudoephedrine.
3. Agents With Mixed Mechanism: Ephedrine, Metaraminol
B) Adrenergic Antagonists:
1.Alpha Adrenergic Blockers: Tolazoline, Phentolamine, Phenoxybenzamine, Prazosin.
2. Beta Adrenergic Blockers: Propranolol *, Atenolol *, Carvedilol
Cholinergic System- Introduction, Definition, Classification, Receptor (with its types & location & action), neurotransmittor present in it, Cholinesterase & its general introduction & action.
A) Cholinergic Drugs and Related Agents: Classification, chemical name, chemical structure (of compounds with * mark), uses, stability and storage conditions, different types of formulation & their popular brand names)
1. Direct Acting Agents: Acetylcholine*, Carbachol, And Pilocarpine,
2. Cholinesterase Inhibitors:
Neostigmine*, Edrophonium Chloride, Tacrine Hydrochloride, Pralidoxime Chloride, Echothiopate lodide
Pulmonary drug delivery system M.pharm -2nd sem P'ceutics
Autonomic Nervous system
1. DRUGS ACTING ON AUTONOMIC NERVOUS SYSTEM
Presented by:- Shalini N. Barad
Lecturer,
Appasaheb Birnale College
of Pharmacy
2. Drugs Acting on Autonomic Nervous System
[Study of the following category of medicinal compounds with
respect classification, chemical name, chemical structure
(compounds with * mark) uses, stability and storage conditions,
different types of formulation & their popular brand names]
A) Sympathetic System
1. Sympathomimetic Agents:
a) Direct Acting: Nor Epinephrine", Epinephrine, Phenylephrine,
Dopamine*, Terbutaline, Salbutamol (Albuterol), Naphazoline*,
Tetrahydrozoline.
b) Indirect Acting Agents: Hydroxy Amphetamine,
Pseudoephedrine.
c) Agents With Mixed Mechanism: Ephedrine, Metaraminol
2. Adrenergic Antagonists:
1) Alpha Adrenergic Blockers: Tolazoline, Phentolamine,
3. B) Parasympathetic System
1. Cholinergic Drugs and Related Agents:
a) Direct Acting Agents: Acetylcholine*, Carbachol, And
Pilocarpine,
b) Cholinesterase Inhibitors: Neostigmine*,
Edrophonium Chloride, Tacrine Hydrochloride,
Pralidoxime Chloride, Echothiopate lodide
24. Adrenergic Drugs:-
These are the drugs which mimics the action like
sympathetic Nervous system.
Drug which produces similar action to adrenaline are called
as
Sympathomimetics
Adrenergic
Adrenomimetics
Adrenergic stimulants
25. Classification of Adrenergic Drugs :-
Catecholamine :- Adrenaline, Nor-adrenaline.
Non catecholamine :-
1. Containing Phenylethylamine group:-
a) With Phenolic group :- salbutamol, Phenylethyline.
b) Without Phenolic Hydroxy group :- Ephedrine.
Aliphatic group :- Cyclopentamine.
Imidazoline group :- Naphazoline.
26.
27. 1. Nor-Epinephrine (Nor-Adrenaline) : Nor-Epinephrine is a
naturally occurring catecholamine hormone that functions as a
neurotransmitter in the sympathetic nervous system.
MF: C8H11O3
Structure:
Chemical Name: 1-(3,4 Dihydroxy phenyl)-2-amino ethanol
28. Uses:
1) To treat life threatening blood pressure in myocardial shock.
2) As vasoconstrictor in some local anaesthetic solutions for dental
use.
3) Used during CPR (cardio-pulmonary resuscitation)
Stability and storage: Solutions of nor-epinephrine can be store up
to two months (avoid light). The brand Levophed solution store
temperature (20°C to 25°C) and protect from light.
Formulation: Injection, 1 mg/ml concentrate solution for Infusion.
Brands Name: Levarterenol, Levophed bitartrate.
29. 2. Epinephrine (Adrenaline):
MF: C9H13O3
Uses:
1) Used to treat very serious allergic reactions to insect stings/bites,
foods other substances.
2) It acts quickly to improve breathing, stimulate the heart, raise a
dropping blood pressure.
3) Use on reverse hives, and reduce swelling of the face, lips, and
throat.
4) It is used in inhibiting uterine contraction.
5) It is used in the treatment of open-angle glaucoma.
Stability and storage: It should be stored in a cool and dark place at
room temp between 15-25°C. Store in an insulated wallet if the
temperature is warmer than than 25°C or colder than 15°C or if they are
carried in a bag which can get warmer than 25°C colder than 15°C.
Formulation: Topical Cream, Solution, Eye drop.
Brand Name: Adrenalin, EpiPen,, Auvi-Q, EpiPen 2-Pak, Glaucon,
30. 3. Phenylephrine:
Molecular Formula: C9H13NO2
Uses:
1) It is used to relieve nasal congestion (discomfort caused by colds,
allergies, and hay fever)
2) It can be used topically to prevent symptoms of hemorrhoids.
3) It is used as an eye drop as mydriatic (to dilate the pupil to
facilitate visualization of the retina).
Stability and Storage:
It gradually darkens on exposure to air & light. Presence of metal
also causes discolouration.
Hence it is stored in tightly-closed light resistant container.
33. Uses:
1) For the treatment of hypotension, low cardiac output,
2) Used to increase mean arterial pressure in septic shock
patients.
3) It improves blood flow to the kidneys.
Storage and stability: Dopamine hydrochloride 0.5 mg/ml in
isotonic glucose solution is stable when protected from light
for 1 week at 25 °C or 60% relative humidity and
for 3months at 4°C/ambient humidity in Codan and Braun
syringes.
Formulation: Dopamine Hydrochloride Injection USP.
Brands Name: Intropin, Dopastat, Revimine.
34. 5. Terbutaline
Stability and Storage :It gradually darkens on exposure to air
and light. Presence of metal an discolouration. Hence, it is stored
in tightly-closed, light-resistant container.
Pharmaceutical formulation: TAB/INJ :- USP
Uses:
1) It is used to treat bronchospasm in bronchial asthma and in
chronic bronchitis. Or (It is used to prevent and treat wheezing,
shortness of breath, and chest tight caused by asthma, chronic
bronchitis, and emphysema).
2) In emergency, treat cardiotoxic shock states, heart block or
severe bradycardia.
Brand Names: Bricanyl, Terbutaline, Bricarex. Misthaler,
Bricanyl.
35. 6. Salbutamol (Albuterol)
Stability and Storage : It is light-sensitive and hence it is stored in
well-closed, light-resistant containers.
Uses:
1) It is mainly used to treat bronchospasm in bronchial asthma and
in chronic bronchitis.
2) In emergency, it is used to treat cardiotoxic shock states, heart
block or severe bradycardia.
3) It is also used in the prevention of premature labour.
Formulations: Tab:-BP, Syrup:- BP, Aerosol:- BP, Inj :- BP
Brand Names: Asthalin, Bronkolax, Albutamol, Croysal, Ventrolin.
36. 7. Naphazoline:
MF: C14H14N2
Structure:
Chemical Name : 2-(1-naphthylmethyl)-2-imidazoline nitrate.
Storage: Store in dropper bottle at room temperature between 20-
25oC away from moisture & sunlight.
37. Uses:
1) It is used for their vasoconstrictive effects as nasal and
ophthalmic deconge
ii) Naphazoline is indicated for use as OTC eyedrops for ocular
vasoconstrictor nasal preparation for nasal congestion.
Pharmaceutical Formulations : solution, Eye drops, Ear drops,
ointment
Band Names: Privine, Naphcon, Naphcon A, Opcon-A, Vasocon,
Visine-A
38. 8. Tetrahydroyzoline:
Storage & Stability: Drops should be generally stored in a cool
dry places.
Uses:
(1) It is used as an ocular and nasal decongestant.
(ii) Tetrahydroyzoline is found in a wide array of over-the-counter
eye drops
(iii) It is also found in combination products with other lubricants and
spray.
Formulations : Eye & Ear drops
Brands: Tyzine, Visine
39. Indirect Acting:
1. Hydroxy amphetamine:
Molecular Formula: C9H13NO
Storage and stability: Store at 20 to 25°C and protect from light
Exclude the reach of children.
Uses:
(1) It is indirect sympathomimetic agent which causes dilation of the
eye pupil before diagnostic test.
(ii) As eye drop is the diagnosis of Horner's syndrome which is
characterized by nerve lesions.
Formulations : Eye drops and Ointments
Brand Name :Paremyd.
40. 2. Psuedoephedrine:
MF: C10H15NO
Stability and Storage : It gradually decomposes on exposure to
light. Hence, it should be stored in tigh closed, light-resistant
containers.
Uses: It is used as:
(1) Nasal decongestant (to treat nasal congestion).
(ii) Bronchodilator in bronchial asthma.
Pharmaceutical Formulations :elixir, tablets, capsules, syrup,
cream, gel, ointments.
Brand Name: Actifed, Advil, Claritin, Tylenol
41. Mixed Acting:
1.Ephedrine:
MF: C10H16NO
Stability Storage:
It is stored in tightly closed, light-resistant containers.
Used: It is used to treat
1) Asthma (due to bronchodilator action).
2) Nocturnal enuresis in children (as it constrict urinary bladder)
3) Nasal congestion.
4) Narcolepsy (tendency to go to sleep)
Formulations: Injection, Tablets, Capsule
Brand names: Ephedrex, Asthamcure
42. 2. Metaraminol:
MF: C9H13NO2
Uses :
(1) It is used parenterally as a vasopressor in the treatment and
prevention of the acute hypotensive state occurring with spinal
anaesthesia.
(ii) It also has been used to treat severe hypotension brought on by
other traumas that induce shock.
(iii) It works by reducing swelling and constricting blood vessels in the
nasal passages and widening the lung airways.
Storage: Store at 25°C excursions permitted to 15-30°C. Store
container in carton until contents have been used. Protect from light
and freezing.
Formulations: Injection.
Brand Name: Aramine
43. Anti-adrenergic drugs :-
Drug which block the adrenergic receptor, doesn’t
allowed to bind the adrenaline or noradrenalin are
called as anti-adrenergic drugs.
Adrenergic blockers :-
α antagonist -
β antagonist
44. Alpha (a)-Adrenergic Blockers: These drugs inhibit adrenergic
responses mediated through the a-adrenergic without affecting
those mediated through B-receptors.
1. Equilibrium type
B-Haloalkyl amines: Phenoxybenzamine.
2. Equilibrium type (competitive)
(a)Non selective:
Imidazolines: Tolazoline, Phentolamine
(b) al selective: Prazosin,
(c) a2 selective: Yohimbine
45. Cholinergic drugs
Cholinergic drugs which produces similar action of
acetylcholine are called as cholinergic drugs.
Cholinergic drugs
Parasympathomimitics
Cholinomimetics
50. Anticholinesterase:-
There are two types of cholinesterase i.e.
acetylcholinestearase and butylcholinestarase.
The enzyme, cholinesterase, catalyze the hydrolysis of
acetylcholine to choline & acetic acid at or near the
site of libration.
Thus acetylcholine is deactivated.
The drug that inhibit the action of cholinesterase and
prolong the life of acetylcholine are called as
anticholinesterase .
These drugs produce similar Pharmacological effect to
that of acetylcholine, hence they are called indirect
51. Classification of cholinergic drugs:-
A) Cholinergic agonist :- (Direct acting)
Esters of choline – acetylcholine, carbachol
Alkaloids - pilocarpine
B)Indirect acting cholinergic agonist (cholinesterase
inhibitors or anticholinesterase):- Neostigmine,
Physostigmine.
53. • Uses
1) Used to obtain miosis of the iris in seconds after
delivery of the lens in cataract surgery.
2) Used in penetrating keratoplasty (especially corneal
transplantation.), iridectomy (the surgical removal of
part of the iris of the eye.)
3) It is also used in anterior segment surgery where
rapid miosis may be required.
• Storage and stability:
Acetylcholine solution stored at 25°C was stable for
about 28 days, after such time, modest breakdown
occurs.
At a temperature of 50°C, ACh showed a rapid
56. 2. Carbachol :
• Uses:
1) It is used to reduce intraoccular pressure
elevations in the first 24 hours after cataract
surgery.
2) Carbachol is a miotic and has been used to reduce
the intraoccular tension of glaucoma.
3) Carbamoylcholine is used to induce miosis for
surgery.
4) Carbachol is used during ocular surgery,
• Pharmaceutical Formulations :
(i) Carbachol Tablet.
(ii) Carbachol Liquid.
(iii) Carbachol Solution.
57. Brand Name: Carbastat and Miostat.
Storage & Stability: Store in refrigerator at 4oC.
Stock solution are stable for 6 month at 4oC
58. 3) Pilocarpine:
• Stability:- hygroscopic, affected by light, with acid &
alkali undergo epimerization stable at pH 4-5.
• Storage :- Stored in Well tightly Closed Amber colour
Container.
Uses: It is used as
1) Miotics (counteract mydriasis).
2) Reduce intraocular pressure in glaucoma.
3) For diagnosis of Adie’s pupil.
4) For adjustment of near vision of eye .
5) To counteract anticholinergic side effect (dryness of
mouth, constipation, and impaired vision of eye)
62. Stability :- affected by light and atmospheric O2.
• Storage :- WTC Amber Container.
• Uses: It is used to treat-
1) Myasthenia gravis.
2) Paralytic ileus.
3) Post operative urinary retention.
4) To promote expulsion of intestinal flatus before
radiography of kidney, uterus.
5) To antagonize muscular relaxation due to curare like
drugs or muscle relaxants used in anesthesia.
6) To diagnose myasthenia gravis.
65. 2) Edrophonium Chloride:
• Uses:
(1) Edrophonium chloride is recommended for
diagnosis of myasthenia gravis.
(i) Edrophonium chloride brings about a rapid increase
in muscle strength with significant side effects.
(iii) It may also be used for evaluating emergency
treatment in myasthenic crises
(iv) To treat neuromuscular blockade
(v) To treat respiratory depression.
66. Storage and stability: should be stored controlled
room temperature 15-30oC
Formulations: Injection, Ointment
Brands Name: Reversol, Tensilon,
67. 3) Tacrine:
• Use:
1. For the treatment of mild to moderate dementia
including Alzheimer's type
• Storage and stability: should be stored in well
closed air tight container at controlled room
temperature 20-25oC
• Pharmaceutical Formulations: Tacrine
hydrochloride capsule, tablet
• Brand Names: THA Cognex, Sugamadex
68. 4) Pralidoxime Chloride:
• Uses:
1) Pralidoxime chloride is used as an antidote for poisoning by parathion
and related pesticides.
2) It may be effective against some phosphates that have quaternary
nitrogen.
3) It is also an effective antagonist for some carbamates, such as
neostigmine, methyl sulfate and pyridostigmine bromide.
• Storage: Store in well closed air tight container (protected from
moisture).
70. 5) Echothiopate lodide:
• Uses:
(i) It is used in the treatment of subacute or
chronic angle-closure glaucoma
(ii) It is also used as a miotic in the treatment of
glaucoma.
(iii) To correct accomodative esotropia,
• Storage: Store under refrigeration (2° to 8°C)
![Drugs Acting on Autonomic Nervous System
[Study of the following category of medicinal compounds with
respect classification, chemical name, chemical structure
(compounds with * mark) uses, stability and storage conditions,
different types of formulation & their popular brand names]
A) Sympathetic System
1. Sympathomimetic Agents:
a) Direct Acting: Nor Epinephrine", Epinephrine, Phenylephrine,
Dopamine*, Terbutaline, Salbutamol (Albuterol), Naphazoline*,
Tetrahydrozoline.
b) Indirect Acting Agents: Hydroxy Amphetamine,
Pseudoephedrine.
c) Agents With Mixed Mechanism: Ephedrine, Metaraminol
2. Adrenergic Antagonists:
1) Alpha Adrenergic Blockers: Tolazoline, Phentolamine,](data:image/gif;base64,R0lGODlhAQABAIAAAAAAAP///yH5BAEAAAAALAAAAAABAAEAAAIBRAA7)