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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5265_Библиотеки_им_академика_М_И_Перельмана.pdf
Drugs Acting on Autonomic Nervous System 177
Marketed Preparations:
➢ Adrenaline Epinephrine Injection – Keshavdas & Sons Pharmaceutical Traders
➢ Epinephrine Injection – Maya Biotech Pvt. Ltd.
Officials:
➢ Adrenaline, I.P.
➢ Adrenaline Bitartrate, I.P.
6.1.3 Phenylephrine
Brand Names: Nasop, Sudafed PE, Sudogest PE
Phenylephrine is a member of phenyl ethanolamines. It is a direct-acting sympathomimetic
amine chemically related to adrenaline and ephedrine with potent vasoconstrictor property. The
chemical structure of Phenylephrine is:
Chemical Name: 3-[(1R)-1-hydroxy-2-(methylamino) ethyl] phenol
Properties: Phenylephrine hydrochloride is an odorless white microcrystalline powder, bitter
taste. It is very soluble in water, freely soluble in ethanol, and insoluble in chloroform and ethyl
ether. Phenylephrine hydrochloride is sensitive to light.
Uses:
➢ Phenylephrine is used as a decongestant to dilate the pupil to increase blood pressure.
➢ It is used in the treatment of nasal congestion caused by colds, allergies, and hay fever.
➢ It is used to relieve hemorrhoids (piles).
Dosage Forms:
➢ Oral liquid (2.5 mg/5 ml)
➢ Oral tablet (10 mg)
➢ Oral tablet, chewable, extended release (tannate 10 mg)
➢ Oral tablet, disintegrating (10 mg).
Stability and Storage: It should be stored in sealed vial at room temperature. Protect from light.
Dry a portion at 105°C for 2 hours before using. Use promptly. Discard unused material.
178 Text Book of Pharmaceutical Chemistry
Marketed Preparations:
➢ FRENIN (Phenylephrine HCL Injection) – Genex Pharma
➢ Phenylephrine HCL Injection, USP – Meitheal Pharmaceuticals Inc.
➢ SINERA TAB – Tanishq Life Care
6.1.4 Dopamine
Brand Name: Intropin
Dopamine is catechol in which the hydrogen at position 4 is substituted by a 2-aminoethyl
group. It is a naturally occurring catecholamine formed by decarboxylation of dehydroxy phenyl
alanine and a precursor of norepinephrine and epinephrine. The chemical structure of Dopamine
is:
Chemical Name: 4-(2-aminoethyl) benzene-1,2-diol
Properties: Dopamine (hydrochloride) is soluble in organic solvents such as ethanol, DMSO and
dimethyl formamide (DMF).
Uses:
➢ Dopamine is used for the treatment of low blood pressure.
➢ It is used for low cardiac output and also helps in improving blood flow in the kidneys.
➢ It is used in poor blood flow to vital organs.
➢ It is used in some cases of septic shock.
➢ It is used in trouble breathing.
Dosage Forms: Dopamine is available in Infusion solution and in Injectable solution.
Stability and Storage: Keep away from direct heat, air and light as it may damage the medicines.
The exposure of medicine may cause some harmful effects. The medicine must be kept in a safe
place and out of children’s reach. It should be kept at room temperature between 68°F and 77°F
(20°C and 25°C).
Marketed Preparations:
➢ Dopar (Dopamine Hydrochloride) – Samarth Life Sciences Pvt. Ltd.
➢ DOPADIC (Dopamine Injection 200 mg/5 mL) – Caspian Tamin Pharmaceutical Co.
➢ Resdop 200 mg/5 mL (Dopamine Hydrochloride Injection) – Health Biotech Ltd.
Drugs Acting on Autonomic Nervous System 179
6.1.5 Terbutaline
Brand Names: Bronclyn, Brethine, Bricanyl, Brethaire, Marex, Terbulin
Terbutaline is a drug of class phenyl ethanolamines that is catechol substituted at position 5
by a 2-(tert-butyl amino)-1-hydroxyethyl group. It contains a stereo center and consists of two
enantiomers but only the (–)-enantiomer of terbutaline is pharmacologically active. The chemical
structure of Terbutaline is:
Chemical Name: 5-[2-(tert-butylamino)-1-hydroxyethyl] benzene-1,3-diol
Uses:
➢ Terbutaline is used in the treatment of wheezing and shortness of breath from lung
problems.
➢ It is used in the treatment of chronic obstructive pulmonary disease.
➢ It is used in the treatment of bronchitis.
➢ It is used in the treatment of emphysema.
➢ It is used for treating asthma and other diseases of the airways.
Properties: Terbutaline is a white to gray-white, crystalline powder; nearly odorless or with the
faint odor of acetic acid. It has a slightly bitter taste. It has a melting point of 247°C. It is soluble
in water and in 0.1 N hydrochloric acid, slightly soluble in alcohol (ethanol) and methanol, and
practically insoluble in chloroform and ether.
Dosage Forms: Terbutaline comes as an oral tablet and as an intravenous (IV) form.
Stability and Storage: Terbutaline should protect from light by storing vials at 15°C to 30°C in
containers with tight-fitting lids. Discolored solutions of terbutaline sulfate should not be used.
Sterile products must be prepared according to USP, Sterile Drug Products for Home Use.
Officials:
➢ Terbutaline Sulphate, I.P.
➢ Terbutaline Sulphate Inhaler, I.P.
➢ Terbutaline Sulphate Injection, I.P.
➢ Terbutaline Sulphate Tablets, I.P.
Marketed Preparations:
➢ SVCOF-BR (Terbutaline 1.25 mg, Bromhexine HCL 4 mg) – SVR Healthcare
➢ PULMOXCEL (Terbutaline sulphate) - Hizon Laboratories
180 Text Book of Pharmaceutical Chemistry
6.1.6 Salbutamol
Brand Names: Airomir, Combivent, Proair, Proventil, Ventolin, Xopenex
Salbutamol, also referred to as Albuterol and sold among other brand names as Ventolin, is a
member of phenyl ethanolamines, a secondary amino compound and a member of phenols. It is
formulated as a racemic mixture of the R- and S-isomers. The R-isomer has 150 times greater
affinity than the S-isomer and the S-isomer has been associated with toxicity. The chemical
structure of Salbutamol is:
Chemical Name: 4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl) phenol
Properties: Salbutamol occurs as white or almost white, crystalline powder, clear solution in
methanol, very pale clear yellow solution. It is sparingly soluble in water, soluble in
ethanol (96%) and slightly soluble in ether.
Uses:
➢ Salbutamol is used to alleviate symptoms such as coughing, wheezing, and feeling
breathless due to asthma. This works by relaxing the airway muscles in the lungs, making
it easier to breathe.
➢ It is used for the relief of bronchospasm in bronchial asthmas of all types.
➢ It is used in chronic obstructive pulmonary disease.
➢ It is used in rescue inhalers (short-term bronchodilators to alleviate asthma attacks).
➢ Intravenous Salbutamol can be used as a tocolytic to relax the uterine smooth muscle to
delay premature labor.
➢ It may also be used to treat high blood potassium levels and acute hyperkalemia.
➢ It is used in Emphysema.
Stability and Storage: Store the salbutamol at room temperature only and try to keep away
from moisture, heat and light. Do not freeze it. Dispense in tight, light-resistant containers.
Inhaler store at controlled room temperature, 25°C; excursions permitted to 15°C-30°C.
Marketed Preparation:
➢ Samol 4 (Salbutamol BP 4 mg) – Cipla Pvt. Ltd.
Officials:
➢ Salbutamol, I.P.
➢ Salbutamol Inhaler, I.P.
➢ Salbutamol Sulphate, I.P.
➢ Salbutamol Sulphate Injection, I.P.
➢ Salbutamol Sulphate Syrup, I.P.
➢ Salbutamol Sulphate Tablets, I.P.
Drugs Acting on Autonomic Nervous System 181
6.1.7 Naphazoline
Brand Names: AK-Con, Albalon, Allersol, Clear Eyes, Clear Eyes + Redness Relief, Naphcon,
Redness Relief Eye Drops.
Naphazoline is an imidazole derivative and a direct-acting sympathomimetic amine with
vasoconstrictive activity. The chemical structure of Naphazoline is:
Chemical Name: 2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole
Uses:
➢ Naphazoline is used as a decongestant and a vasoconstrictor.
➢ It is a decongestant used to relieve redness, puffiness and watery eyes caused by colds,
allergies or eye irritations.
Dosage Forms:
➢ Ophthalmic gel forming solution (0.012%)
➢ Ophthalmic solution (0.012%; 0.012% with glycerin; 0.1%)
Stability and Storage: Keep in a cool, well ventilated place away from heat sources and direct
sunlight. Keep container closed when not in use. The drug should be kept at room temperature
between 68°F and 77ºF (20°C and 25°C) in dry protected location to prevent any moisture
contact.
6.1.8 Tetrahydrozoline
Brand Names: Colirio Ocusan, Visine
Tetrahydrozoline, also known as Tetryzoline, is a derivative of imidazoline which is found in
over-the-counter eye drops and nasal sprays. The chemical structure of Tetrahydrozoline is:
Chemical Name: 2-(1,2,3, 4-tetrahydronaphthalen-1-yl)-4,5-dihydro-1H-imidazole; hydrochloride
Properties: It occurs as white, odorless solid, melts at about 256°C with decomposition. It is
freely soluble in water and in alcohol; very slightly soluble in chloroform; and practically
insoluble in ether.
182 Text Book of Pharmaceutical Chemistry
Uses:
➢ Naphazoline is used as an ocular and nasal decongestant.
➢ It is indicated for the temporary relief of discomfort and redness of the eye due to minor
eye irritations as monotherapy.
➢ It is used for the temporary relief of burning and discomfort due to dryness of the eye or
exposure to wind or sun.
Dosage Forms:
➢ Available as tetrahydrozoline hydrochloride
➢ Dosage expressed in terms of the salt, ophthalmic solution (0.05%)
Stability and Storage: Store the medicine in a closed container at room temperature, away from
heat, moisture and direct light.
Marketed Preparations:
➢ Vizoline (Tetrahydrozoline HCL) Ophthalmic Sol USP – Optica Pharmaceutical (P) Ltd.
➢ Histazolin Eye Drops 15 ml (Sodium Cromoglycate and Tetrahydrozoline) – Remington
Pharma
➢ Efemyo Eye Suspension drops 10 ml (Fluorometholone + Tetrahydrozoline) – Orchidia
Pharmaceutical Industries
INDIRECT ACTING AGENTS
6.1.9 Hydroxy Amphetamine
Brand Name: Paremyd
Hydroxyamphetamine is a derivative of amphetamines. It is indirect sympathomimetic agent
which causes dilation of the eye pupil before diagnostic test. The chemical structure of
Hydroxyamphetamine is:
Chemical Name: 1-(4-hydroxyphenyl) propan-2-ylazanium
Uses:
➢ Hydroxyamphetamine is used medically in eye drops to dilate the pupil (mydriasis).
➢ It is used to dilate pupil in inflammatory condition.
➢ It is used in post-surgery situations.
Drugs Acting on Autonomic Nervous System 183
Stability and Storage:
Store the medicine in a closed container at room temperature, away from heat, moisture and
direct light. Store between 20°C and 25°C (68°F and 77°F). Protect from light.
6.1.10 Pseudoephedrine
Brand Names: Chlor Trimeton Nasal Decongestant, Contac Cold, Drixoral Decongestant
Non-drowsy
Pseudoephedrine is a secondary alcohol, a secondary amino compound and member of the class
of phenyl ethanolamines. It is a diastereomer of ephedrine with sympathomimetic property. It
occurs naturally in plants of the genus Ephedra. Pseudoephedrine is a mixed-acting decongestant.
The chemical structure of Pseudoephedrine is:
Chemical Name: (1S,2S)-2-(methylamino)-1-phenylpropan-1-ol
Properties: Pseudoephedrine hydrochloride occurs as fine, white to off-white crystals or powder,
having a faint characteristic odor. It is very soluble in water, freely soluble in alcohol, and
sparingly soluble in chloroform.
Uses:
➢ Pseudoephedrine is used as a decongestant (sympathomimetic).
➢ It reduces tissue hyperemia, edema, and nasal congestion commonly associated with
colds or allergies, hay fever and bronchitis).
➢ It is used either as oral or as topical decongestant.
➢ It is used in the treatment of nasal congestion, sinus congestion and eustachian tube
congestion.
➢ It is indicated for the treatment of vasomotor rhinitis.
➢ It is used in the treatment of allergic rhinitis, croup, sinusitis, otitis media, and
tracheobronchitis.
Dosage Form: Available as pseudoephedrine hydrochloride; dosage expressed in terms of the
salt. Tablet, film coated extended release.
Stability and Storage: Store the medicine in a closed container at room temperature, away from
heat, moisture, and direct light, keep from freezing. Conventional tablets should be stored at
temperature: 15°C to 25°C in a dry place. Extended-release tablets should be stored at 15°C to
25°C in a dry place.
184 Text Book of Pharmaceutical Chemistry
Marketed Preparations:
➢ Sudafed (Pseudoephedrine HCl 120 mg; ext-rel caplets) – McNeil Consumer Healthcare
➢ Wal-phed (Pseudoephedrine hydrochloride 30 mg) – Walgreen Company
➢ Pseudoephedrine Hydrochloride – CVS Pharmacy
Officials:
➢ Pseudoephedrine Hydrochloride, I.P.
➢ Pseudoephedrine Hydrochloride Syrup, I.P.
➢ Pseudoephedrine Hydrochloride Tablet, I.P.
6.1.11 Ephedrine
Brand Names: Akovaz, Bronkaid, Corphedra, Emerphed, Primatene, Rezipres
Ephedrine is a phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl
group at the amino nitrogen, and a methyl and a hydroxy group at position 2 and 1 respectively.
Chemically, ephedirine can exist as four stereoisomers. The chemical structure of Ephedrine is:
Chemical Name: (1R,2S)-2-(methylamino)-1-phenylpropan-1-ol
Properties: Ephedrine exists as colorless crystals or white, crystalline, orthorohombic needless or
powder, odorless, with a bitter taste. It is freely soluble in water, sparingly soluble in alcohol,
very slightly soluble in chloroform, and practically insoluble in ether.
Uses:
➢ Ephedrine is used to prevent low blood pressure during anesthesia.
➢ It is used for asthma, narcolepsy and obesity.
➢ It is used to decrease motion sickness.
➢ It is used in congenital myasthenic syndrome (neuromuscular disorder).
➢ It is used for allergies, nasal congestion, common cold and headache.
Dosage Form: Ephedrine Sulphate Injection, USP is a sterile solution of 50 mg ephedrine sulfate
in water for injection (Rezipres). The usual parenteral dose is 25 to 50 mg given subcutaneously
or intramuscularly. Intravenously, 5 to 25 mg may be administered slowly, repeated in 5 to 10
minutes, if necessary.
Stability and Storage: Store at room temperature, between 59°F and 77°F (15°C and 25°C),
away from heat, moisture and light. Do not store above 25°C. Store it in the original container in
order to protect from light. Keep ephedrine out of the reach of children and away from pets.
Drugs Acting on Autonomic Nervous System 185
Marketed Preparations:
➢ Ephedrine HCl 30 mg – Delphis Pharma
➢ Ephedrine sulfate intravenous – Nexus Pharmaceuticals
➢ Ephedrine HCL Tablets – AdvaCare Pharma
Officials:
➢ Ephedrine, I.P.
➢ Ephedrine Hydrochloride, I.P.
➢ Ephedrine Hydrochloride Oral Solution, I.P.
➢ Ephedrine Hydrochloride Tablet, I.P.
6.1.12 Metaraminol
Brand Name: Aramine
Metaraminol, also known as Aramine, is a member of the class of phenylethanolamines that
is 2-amino-1-phenylethanol substituted by a methyl group at position 2 and a phenolic hydroxy
group at position 1. The chemical structure of Metaraminol is:
Chemical Name: 3-[(1R,2S)-2-amino-1-hydroxypropyl]phenol
Properties: It occurs as a white, crystalline powder. It is highly water soluble, slightly soluble
in alcohol, and practically insoluble in chloroform and in ether.
Uses: Metaraminol is used to treat a number of conditions including:
➢ Treatment of the acute hypotensive state occurring with spinal anesthesia.
➢ Treatment of hypotension due to hemorrhage
➢ Used in surgical complications, and shock associated with brain damage due to trauma
or tumor.
➢ Used in the treatment of priapism.
Dosage Form: Metaraminol 10 mg/mL solution for Injection/Infusion
Storage and Stability: Store at 25°C; excursions permitted to 15-30°C. Store the container in
carton until contents have been used. Protect from light. Protect from freezing.
Marketed Preparations:
➢ Metaraminol-Meta – DMS Pharma
➢ Metaraminol Injection B.P. – SG Pharma
186 Text Book of Pharmaceutical Chemistry
6.2 ADRENERGIC ANTAGONISTS
Adrenergic nervous system is the part of the autonomic nervous system that uses epinephrine
or norepinephrine as its neurotransmitter. The word adrenergic means working on adrenalin
(epinephrine) or noradrenalin (norepinephrine) or on their receptors.
Adrenergic receptors subtypes include α
1
, α
2
, β
1
, β
2
and β
3
receptors. Adrenergic drugs or
(Adrenergic agonist) are a broad class of medications that bind to and activate adrenergic
receptors throughout the body. Adrenergic antagonists are group of drugs that inhibits the
function of adrenergic receptors.
Adrenergic antagonists are group of drugs that inhibit the action of adrenergic receptors,
i.e., adrenaline (epinephrine) and noradrenalin (norepinephrine). Adrenergic antagonists (Adreno
blockers) are broadly used in the treatment of cardiac diseases.
Alpha-adrenergic Blockers
Alpha-adrenergic Blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a
class of drugs that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Alpha-1 (α
1
)
blockers act on α
1
-adrenoceptors while Alpha-2 (α
2
) blockers act on α
2
-adrenoceptors. Alpha-
blockers are medications used to treat a small range of diseases such as treatment of essential
hypertension, benign prostatic hyperplasia (BPH), pheochromocytoma, Reynaud’s disease
and erectile dysfunction.
6.2.1 Tolazoline
Tolazoline is a drug of the class imidazoles that is 4,5-dihydro-1H-imidazole substituted by a
benzyl group. Also known as priscoline, it was used in the treatment of persistent pulmonary
hypertension. It is a non-selective competitive α-adrenergic receptor antagonist. The chemical
structure of Tolazoline is: