Clinical Use Of Agents

Amphetamine Metabolite Cycle

Psychostimulants generally increase the level of activity, alleviate fatigue, increase alertness, and elevate mood (or cause euphoria in high doses). Unfortunately, the ability to produce euphoria leads these compounds to have a high potential for abuse and dependency. The principal clinical indications for psychostimulants are in the treatment of attention deficit hyperactivity disorder (ADHD) and the sleep disorder known as narcolepsy. A less commonly recognized use, but one that' is gaining...

Other Side Effects

The most common side effect of long-term narcotic analgesia is constipation plus other gastrointestinal (GI) effects collectively referred to as opioid bowel dysfunction. The frequency of these side effects is very high 40-50 or more in patients receiving opioids (34-36) and can become the limiting factor in opioid use. These effects are mediated predominantly by jit receptors in the bowel (23).The effects begin with delayed food digestion in the small intestine and...

Websites

The following are a number of selected websites that pertain to sleep disorders and or sedative-hypnotics. diagnostics sleep sleep4.html diagnosis and therapy of sleep disorders sleep disorders and their treatment iac 100547893 sleep disorders and their treatment html abuse of and intoxication by psychotropic drugs including sedative-hypnotics http www.acnp.org G4 GN401000173 CH169.html mechanism of action and pharmacology of barbiturates html abuse of and intoxication by psycho-tropic drugs...

Molecular Basis For The Side Effects Of Anticholinergics

The most widely used mode cf approach in the design cf anticholinergics is based on the use cf tropine alkaloids as models of prototypes, from which congeners or homologs or analogs have been designed. Tropine alkaloids have many pharmacological activities and interact at many cholinergic sites. In drug design the main purpose is to increase one pharmacological action at one particular site of action while concomitantly suppressing other pharmacological activities at other sites. It is not...

Maoi

Amphetamine Apomorphine GABA GABA-ergic compounds Opioids IL-1 TN Fa Figure 5.8. REM sleep on and off switches. 2. Excitatory Amino Acids EAAs . Excitatory 6. amino acids are claimed to be the principal excitatory transmitters in the reticular formation 34 . EAAs including glutamate are involved in the positive feedback interaction between the cholinergic and the retic- 7 ular neurons. 3. Vasoactive Intestinal Peptide. The peptide is found in the same neurons of the reticular formation where...

Info

2.2.3 Halogenated Sedative-Hypnotics, 208 2.2.4 Heterocyclic Sedative-Hypnotics, 210 . 2.3 Absorption, Distribution, Metabolism, and Elimination, 211 2.3.3 Halogenated Sedative-Hypnotics, 220 2.3.4 Heterocyclic Sedative-Hypnotics, 221 3 Physiology and Pharmacology, 233 3.1.1 Wakefulness and Sleep, 223 3.1.2Sleep Studies, 224 3.1.3States of Sleep, 224 3.1.4Alert Wakefulness, 224 3.1.8 Neurotransmitters and Sleep, 225 3.1.9 Neurotransmitters and REM Sleep in Humans, 225 3.1.10 Nonhypnotic Drugs...

C2h5

Ethosuximide, 5a Methsuximide, 5 b Phensuximide, 5c Phenobarbital, 6 Primidone, 7 cially when initiating or stopping either drug. Likewise, carbamazepine exerts a variable effect on phenytoin levels conversely, carbam-azepine serum levels may also be decreased. Folate deficiency has been noted with long-term phenytoin therapy, given that folate is a cofactor in the metabolism of phenytoin through hydroxylation see metabolism . Similarly, influenza virus vaccine may increase, decrease, or have...

Cinnamon And Mydriasis

Table 3.2 Derivatives of Solanaceous Alkaloids and Their Advantage, if any, of Molecular Modification Ipratropiumb bromide Atropine N-oxide hydrochloride Hyoscyamine hydrobromide Methylatropine nitrate Scopolamine hydrobromide hydrobromide Methscopolamine bromide NF bromide NF Anisotropine methylbromidec 0.5 mg orali.v or s.c. 0.5-1.0 ophthalmic solution 2.5-5.0 mg oral 0.251.0 mg s.c. or i.m. 2-4 mg oral 0.25-0.5 mg s.c. or release of the alkaloid Low systemic absorption Slow release of the...

Structureactivity Relationships

Boat Conformation 180

Examination of the structure-activity relationships SARs of several of the classic stimulants provides not only an understanding of the development of other drugs, but provides important clues as to the underlying mechanisms involved in interaction with the target protein s . The following sections will hopefully illustrate both of these points. There are a number of related structures that are often referred to as amphetamines, although the name amphetamine refers to one specific molecular...

Ch3o

Synthesized within and secreted by the pineal gland. It has a wide variety of biological effects in various species, but in humans its principal effect is the regulation of the body's circadian rhythm sleep-wake cycle . It is well-established that the pineal gland produces and releases melatonin during.the hours of darkness and that the functions of the pineal gland are controlled by light and changes in the duration of the photoperiod 174,175 . There is some evidence that the pharmacological...

Generic For Chloralodol

3-6 p.o divided doses 0.25-0.50 p.o. 5-20 p.o 0.5-2.0p.o. Table 5.5 Halogenated Sedative Hypnotics Chloral hydrate compound with betaine 2-Methyl-2 2,2,2-trichloro-l-hy droxy ethoxy -2-pentanol Ethyl AT- 2,2,2-trichloro-l-hydroxyethyl carbamate ethanol, di-H-phosphate, sodium salt with chloral 2-bromo-2-ethyl-butyryl urea l-chloro-3-ethylpent- l-en-4-yn-3-ol Chloralodol or chlorhexadol Carbochloral Chloralodol or chlorhexadol Carbochloral interactions because benzodiazepines do not induce...

Ch3 C2h5

Barbituric Acid

N- 2- 5-Methoxy-1 H-indol-3 -yl ethyl McNeil J amp J Recordati Italy Zeneca mary metabolic processes that may take place. 1. Oxidation of substituents attached to C5 is the most important pathway of metabolism for the barbiturates. The oxidative processes may yield alcohols, ketones, and car-boxylic acids. For example, pentobarbital is oxidized to a hydroxy compound and a car-boxylic acid 8 as shown in Fig. 5.2. The oxidative process may also yield phenols. If the barbiturate has a phenyl group...

Y

Brotizolam

Metabolism of phenobarbital. determined by redistribution of the drug into inactive storage sites, elimination, and metabolism. The presence of active metabolites contributes heavily to the duration of action of benzodiazepines. Some active metabolites have much longer plasma half-lives than their parent compounds. If the parent drug is not bio-transformed into active metabolites, the duration of action is determined by the rate of elimination of the parent compound. The...

Gastric Secretion Peptic Ulcer and Anticholinergics as Antiulcer Agents

Histamine Gastric Ulcer

The pathophysiologyof peptic ulcer is not fully known and, in the present state of knowledge, it is not possible to present the pertinent normal physiology briefly. For a detailed discussion on the physiology and chemistry of gastric secretion and the pathologic physiology of peptic ulcer, reference should be made to reviews on the subject 1-5 . The following is a brief summary of the gastric secretion and its relationship to peptic ulcer, a knowledge of which is necessary to understand the...

Les Enantiomeres Du Carteolol

Albuterol Sulfate Reaction

Triceuticals on the market whose active ingredient is the adrenergic agonist ephedrine. Pseudoephedrine, the threo diastereomer, has virtually no direct activity on adrenergic receptors but acts by causing the release of norepinephrine from nerve terminals, which in turn constricts blood vessels. Although it too crosses the blood-brain barrier, pseudoephed-rine's lack of direct activity affords fewer CNS side effects than does ephedrine. Pseudo-ephedrine is widely used as a nasal deconges-tant...

History

In 1895 Oliver and Schafer reported 57 that adrenal gland extracts caused vasoconstriction and dramatic increases in blood pressure. Shortly thereafter various preparations of crude adrenal extracts were being marketed largely to staunch bleeding from cuts and abrasions. In 1899 Abel reported 58 isolation of a partially purified sample of the active constituent 2 , which he named epinephrine. Shortly thereafter von F rth 59 employed an alternative procedure to isolate another impure sample of 2...

Ch2oh Structure

Process Production Guanabenz

Reoselective for the active R- - -isomer 1820 , resulting in higher plasma levels of the less active S- -isomerafter oral administration or swallowing of inhaled dosages. Tamsulosin 24 is metabolized by CYP3A4 to both the phenolic oxidation product 75 and deaminated metabolite 76 and their conjugation products 21-23 . The other products generated from the remainder of the drug molecule during formation of 76 were not explicitly identified. Tamsulosin is well absorbed orally and extensively...