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Document Text Contents
Page 165

156 PRINCIPLES OF ORGANIC MEDICINAL CHEMISTRY

C-8—N-CHEMI\CHE11-1.PM5

Adrenaline is available as adrenaline acid tartarate. Adrenaline is a white or creamy
white crystalline and odorless powder. It is slightly soluble in water but freely soluble in min-
eral acids and alkali hydroxides. Adrenaline is insoluble in alcohol, ether and chloroform. It
darkens slowly on exposure to air and light.

Adrenaline is a potent stimulator of both α and β receptors and, as such, its administra-
tion produces effects resembling generalized activation of the sympathetic nervous system
particularly prominent are the actions on the heart and vascular smooth muscle. The occur-
rence of sweating, piloerection and mydriasis depend largely upon the physiological state of
the subject.

Adrenaline is one of the most potent vasopressors known, given by IV route, it evokes a
characteristic rise in blood pressure. The mechanism of the rise in blood pressure with adrena-
line is;

1. Direct myocardial stimulation (positive inotropic effect)

2. An increased heart rate (positive chronotropic effect)

3. Peripheral vasoconstriction

Absorption, fate and excretion. Due to rapid oxidation and conjugation in the GIT
mucosa and liver adrenaline is ineffective after oral administration. Absorption from subcuta-
neous tissues occurs slowly due to local vasoconstriction. Adrenaline is rapidly inactivated in
the body, despite its stability in blood. The liver is rich in both COMT and MAO, however is not
essential in the degradation process. The majority of an administered drug is excreted in the
urine as metabolites.

Uses. The oral intake of adrenaline has no effect. Therefore it has to be administered
parenterally. It is used as sympathomimetic (drugs which support the beating of the heart),
broncholytic (drugs which relax the bronchial muscles) and antiasthmatic (drugs against
asthma). It is also used to prevent bleedings during surgery or in the case of inner organ
bleeding. Because adrenaline leads to constriction of blood vessels, it is administered in combi-
nation with local anesthetics. In this combination, anesthetics have a longer lasting effect and
can be administered in smaller doses.

Page 166

ADRENERGIC DRUGS 157

C-8—N-CHEMI\CHE11-1.PM5

Noradrenaline (Norepinephrine)

Chemistry. Norepinephrine, or l-β-[3,4-dihydroxyphenyl]-α-methyl-aminoethanol is the
chemical mediator liberated at mammalian post-ganglionic adrenergic nerve terminals.
Noradrenaline is available as acid tartarate salt. It is available as odorless, bitter taste, white
crystalline powder. It is soluble in water and slightly soluble in alcohol. Noradrenaline should
be protected from air and light as it darkens on exposure to air and light.

It differs from adrenaline only by lacking the methyl substitution on the aminoethanol
and, as for adrenaline, the l-isomer is pharmacologically active. Noradrenaline constitutes 10-
20% of the catecholamine content of the adrenal medulla and as much as 97% in some
pheochromocytomas. Norepinephrine bitartrate is a water soluble, crystalline monohydrate
salt, which, like adrenaline, it is readily oxidised. It is available for injection as 0.2% bitartrate,
which is equivalent to noradrenaline 0.1%. It is usually given as a central i.v. infusion at a
concentration of 60 µg/ml.

Pharmacological actions. Both adrenaline and noradrenaline are approximately
equipotent at cardiac β1 receptors. Noradrenaline is a potent agonist for α-receptors but has
little action on β2 receptors. However, noradrenaline is somewhat less potent than adrenaline
at most α-receptors.
Dopamine

Chemistry. Dopamine (3,4-dihydroxyphenylethylamine), differs from the other natu-
rally occuring catecholamines, lacking the β-OH group on the ethylamine side chain. It is the
metabolic precursor of noradrenaline and adrenaline and is a central neurotransmitter.

Pharmacology. Dopamine is a substrate for both MAO and COMT and is thus ineffec-
tive orally. It has minimal effects on the CNS, not crossing the blood brain barrier. Dopamine
exerts a positive inotropic effect on the heart, acting at β1 receptors. Dopamine usually in-
creases the systolic and pulse pressures.

Dosage and administration. Dopamine hydrochloride is a water soluble, crystalline,
light and alkali sensitive white powder marketed in solutions of 40, 80 and 160 mg/ml. Dopamine
is effective only by i.v. infusion, when it is usually diluted to 0.8 to 1.6 mg/ml. The usual adult
dose is 2-5 µg/kg/min.

Uses. Acute congestive cardiac failure with imminent renal failure, septic shock,
cardiogenic shock, surgical shock, acute pancreatitis.

ISOPROTERENOL(ISOPRENALINE)

Chemistry. Isoproterenol, or dl-β-[3,4-dihydroxyphenyl]-α-isopropylaminoethanol, is
a synthetic catecholamine acting almost exclusively at β receptors.

Page 330

INDEX 321

C-8—N-CHEMI\INDEX.PM5

Osmotic diuretics, 262

Oxazolidinediones, 106

Oxidation, 44

Oxycodone, 216

Oxymetazoline, 167

Oxymorphone, 215

Oxyphenbutazone, 245

Oxyphencyclimine, 143

Paracetamol, 247

Paraldehyde, 72

Paramethadione, 107

Parasympathetic nervous system, 121

Parathion, 137

Partitioncoefficient, 16

Pentazocine, 224

Pentobarbitone, 67

Pethidine, 219

Phenacemide, 115

Phenacetin, 247

Phenelzine, 100

Phenformin, 279

Phenindamine, 205

Pheniramine, 195

Phenobarbitone, 103

Phenothiazines, 198, 78

Phenoxybenzamine, 178

Phensuximide, 108

Phentolamine, 177

Phenylbutazone, 245

Phenylephrine, 158

Phenylsalicylate, 235

Phenytoin, 104

Pholcodeine, 213

Physico-chemical properties, 14

Physostigmine, 132

Pilocarpine, 130

Piperazines, 200

Piperidolate, 146

Piroxicam, 244

Poldinemethylsulfate, 145

Pioglitazone, 280

Pentazocine, 224

Potassium-sparing diuretics, 268

Pralidoxime, 137

Prazepom, 75

Prazosin, 176

Primidone, 115

Procaine, 255

Prochlorperazine, 80

Procyclidine hydrochloride, 145

Prodrugs, 31

Promazine, 81

Promethazine, 199

Pronethalol, 173

Prontosil, 34

Propanidid, 59

Propantheline bromide, 142

Propionicacid derivatives, 237

Propofol, 60

Propoxyphene, 222

Propylamine derivatives, 195

Propylhexedrine, 164

Propylthiouracil, 288

Protein binding, 27

Psychoactive drugs, 77

Psychotropic drugs, 77

Pyridostigmine, 133

Pyrilamine, 193

C

Quinalbarbitone, 70

Quinazolines, 176

Quinethazone, 266



Ranitidine, 209

Reductive reactions, 47

Ritodrine, 162

Rofecoxib, 248

Rosiglitazone, 280

Repaglinide, 281

Page 331

322 PRINCIPLES OF ORGANIC MEDICINAL CHEMISTRY

C-8—N-CHEMI\INDEX.PM5



Salicylamide, 235

Salicylates, 234

Sedative-hypnotics, 61

Selective serotonin re-uptake inhibitors, 95

Selegiline, 100

Serotonin, 95

Sertraline, 98

Skeletal muscle relaxants, 180

Sodium salicylate, 235

Soft drugs, 40

Solubility, 14

Spiranolactone, 269

Succinimides, 108

Sulfate conjugation, 49

Sulfonyl ureas, 274

Sulindac, 241
Surfaceactivity, 26
Sympathetic nervous system, 122



Temazepam, 75

Terbutaline, 160

Tetrahydrozoline, 165

Thebaines, 218

Thiazides, 265

Thiopentone, 58

Thonzylamine, 194

Thyroid drugs, 282

Thyroid hormones, 282, 283

Thyroxine sodium, 286

Timolol, 172

Tolazoline, 177

Tolbutamide, 275, 276, 277

Torsemide, 263

Tranylcypromine, 100

Triazolam, 76

Trichloroethylene, 56

Triclofos sodium, 73

Tricyclic antidepressants, 91

Trifluoperazine, 80

Trifluopromazine, 81

Trihexyphenidyl hydrochloride, 142

Trimeprazine, 198

Trimethadione, 107

Triprolidine, 197

Tropicamide, 144

Triamterene, 268

Thiazolidinones, 280

%

Urea, 262

"

Valdecoxib, 248

Valproic acid, 116

Venlafaxine, 98

Vigabatrin, 118

5

Xylometazoline, 166

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