Reviews

Eat The Fat Off Review

Eat The Fat Off Review

GrowTaller4U Review

GrowTaller4U Review

Fatlicious Lets You Flush Out Fat Reserves By Following Ketogenic Diet

Fatlicious Lets You Flush Out Fat Reserves By Following Ketogenic Diet

Old School Body Hacks Review

Old School Body Hacks Review

Lose Man Boobs in 30 Days Review

Lose Man Boobs in 30 Days Review

Turmeric with BioPerine Supplements Review

Turmeric with BioPerine Supplements Review

Review: Destroy Depression

Review: Destroy Depression

Peripheral Neuropathy Solution Review

Peripheral Neuropathy Solution Review

Articles

What happens if hypothyroidism is left untreated?

Hypothyroidism is a condition where the thyroid gland produces a little amount of thyroid hormone below the required level needed by our body. Thyroid hormone is important in maintaining and regulating the body&rsquo s metabolism such as core body temperature and energy utilisation by the body&rsquo s tissue. The condition can be diagnosed by using a laboratory test known as Thyroid Function Test. Besides the hormonal imbalances shown by the test, patients with hypothyroidism may also need...

Ketogenic Diet in the 1990s

Use of the ketogenic diet decreased greatly until it received national media attention in October 1994, when NBC-TV's Dateline aired a program on the treatment (7,8,42,63-66). This television program was based on the true story of Charlie, a 2-yr-old with intractable myoclonic, generalized tonic, and tonic-clonic seizures (Fig. 4). A videotape presentation made later summarizes Charlie's condition in 1994 Thousands Fig. 4. Charlie Abrahams, age 4, with his parents Jim and Nancy, as they...

Biopharmaceutics Classification System

The BCS classification system is used to categorize drugs and serves to help anticipate whether drugs will have bioavailability bioequivalence problems. BCS classifies drugs according to their solubility and permeability. A drug is considered to have high solubility if drug substance at the highest dose strength for an immediate release formulation can be dissolved in lt 250 mL of water over a pH range of 1-7.5. A high permeability drug is one that has either complete intestinal absorption fa...

O Factors Affecting Drug Metabolism

Drugs and xenobiotics often are metabolized by several different phase I and phase II pathways to give several metabolites. The relative amount of any particular metabolite is determined by the concentration and activity of the enzyme(s) responsible for the biotransformation. The rate of metabolism of a drug is particularly important for its pharmacological action as well as its toxicity. For example, if the rate of metabolism of a drug is decreased, this generally increases the intensity and...

Caffeine and benzodiazepines

Benzodiazepines are widely used for the treatment of anxiety and insomnia as well as a variety of other disorders. In most countries they are available on medical prescription. Problems of dependence and abuse have been recognized for some time, although the dependence potential of these drugs remains a matter of contention.14 In addition to their anxiolytic and hypnotic effects, benzodiazepines produce sedation, muscle relaxation, and cognitive and psychomotor impairment. A number of studies...

Summary And Conclusion

In the foregoing discussion we have tried to define the nature of OxS and then, using that definition, to assess the status of OxS in diabetes. Based on analysis of various biomarkers of OxS in long-lived proteins, we conclude that OxS is not overtly or systemically increased in diabetes, except at later stages in the development of complications. Metabolic derangements in diabetes lead to an increase in concentration of oxidizable substrates and compromised detoxification pathways. The...

Examples Of Infusion Drugs That Photodegrade

Polyunsaturated fatty acids, commonly used in drug formulations, are particularly susceptible to oxidation, and care must be exercised to minimize degradation in formulations containing high concentrations of, for example, vegetable oils (31). The oxidation of phenothiazines to the sulfoxide involves two single-electron transfer reactions involving a radical cation intermediate the sulfoxide is subsequently formed by reaction of the cation with water (32). The ether group in drugs such as...

Aloe Vera- As A Treatment For Lung Cancer

Aloe (Aloe vera) is a cactuslike plant originally indigenous to Africa. Aloe vera is the most prominent among the more than 300 species belonging to this family. It was widely regarded as a master healing plant in folkloric medicine.149 In the last few decades, aloe has gained popularity as an adjunct treatment to heal burns and side effects following radiation therapy. This important application, which correlates with its traditional usage as a remedy to cuts and burns, has gained momentum...

Occupational Therapy Interventions

Occupational therapy treatment interventions may be classified into three broad categories preparatory methods, purposeful activity, and occupation-based interventions (The American Occupational Therapy Association 2008b) (Table 15.3). Preparatory methods include interventions intended to prepare the client for engaging in activity and may include splinting, edema management, physical agent modality application, and therapeutic exercise (The American Occupational Therapy Association 2008b)....

Sources of leads and drugs

Originally drugs and leads were derived from natural sources. These natural sources are still important sources of lead compounds and new drugs, however the majority of lead compounds are now discovered in the laboratory using a variety of sources, such as local folk remedies (ethnopharmacology), investigations into the biochemistry of the pathology of disease states and high-throughput screening of compound collections (see Chapter 5), databases and other literature sources of organic...

Different Classes Of Heterotrimeric G Proteins And Their Coupling Properties

The different classes of G proteins are defined by their sequence identity as well as their downstream effector coupling specificity. There are over 20 Ga-subunits known to date, and they are divided into four major Ga subfamilies. Because the coupling of the receptor to the different classes of G proteins specifies the signaling pathways that are activated, GPCRs are functionally classified according to their coupling specificity, such as Gs- or Gq-coupled receptors. Several recent reviews...

Reproductive Effects

No studies were located regarding reproductive effects in humans after oral exposure to boron. Animal studies demonstrated that boron can cause injury after intermediate and chronic exposure to the gonads in animals, especially the testes. Impaired spermatogenesis has been reported in rats administered 300 mg boron L as borax (44.7 mg boron kg day) in drinking water for 70 days (Seal and Weeth 1980), but no reproductive effects were evident in rats administered up to 6 mg boron L of borax (0.6...

Opioids Inducing Nausea And Emesis

The main physiological consequence of nausea and emesis is the removal of toxins, which is an important protective reflex mechanism being induced during food intoxication. It however, is also seen after radiation or chemotherapy, after the administration of an opioid-based anesthetic regimen or during long-term therapy for alleviation of chronic pain. About 20 of all patients experience nausea and or emesis after opioid anesthesia. The cause of such reaction is a stimulation of the...

Conversion of Morphine to Heroin Diacetylmorphine

The following is a step-by-step description of morphine extraction in a typical Mainland Southeast Asian laboratory. An empty 55-gallon oil drum is placed on bricks about a foot above the ground and a fire is built under the drum. Thirty gallons of water are added to the drum and brought to a boil. Ten to fifteen kilograms of raw opium are added to the boiling water. With stirring, the raw opium eventually dissolves in the boiling water, while soil, leaves, twigs, and other non-soluble...

Physicochemical drug interactions and incompatibilities

10.1 pH effects in vitro and in vivo 395 10.7 Adsorption of drugs 414 10.2 Dilution of mixed solvent systems 401 10.8 Drug interactions with plastics 417 10.3 Cation-anion interactions 402 10.9 Protein binding 419 10.4 Polyions and drug solutions 405 Summary 425 10.5 Chelation and other forms of Appendix 425 complexation 405 References 429 10.6 Other complexes 410 Further reading 430 This chapter deals with some practical consequences of the physical chemistry of drugs -particularly their...

The Macrophage Theory Of Depression

Of all the endocrine changes that are reported to occur in stress and depression, Cortisol hypersecretion is the most frequently observed. Although hypercortisolaemia can arise as a consequence of an acute stressor, there is a qualitative difference between the circadian pattern of Cortisol secretion in the depressed patient and that observed following exposure to a stressful stimulus. Thus the nadir of the plasma Cortisol concentration occurs some 6 hours earlier in the depressed patient than...

Classification of drugs

Drugs are classified in different ways depending on where and how the drugs are being used. The methods of interest to medicinal chemists are chemical structure and pharmacological action, which includes the site of action and target system. However, it is emphasised that other classifications, such as the nature of the illness, are used both in medicinal chemistry and other fields depending on what use is to be made of the information. In all cases, it is important to bear in mind that most...

Sensory Pathways and GABA

The transmission and perception of pain are complex processes involving both the central and peripheral nervous systems. In general, pain impulses are generated, propagated, and sustained by the liberation of various autocoids, ions, and neurotransmitters at various points between the site of tissue damage, along the afferent sensory fibers, and within the spinal cord and brain. Some endogenous agents, including adenosine and a variety of neuro-peptides, are responsible for initiating,...

Inhibitory and Excitatory Effects of Nociception at the Spinal Cord Level

Within the spinal cord, either an enhancement and or an inhibition of ascending nociceptive afferences come into effect. The spinal cord is also considered as the major site where a number of analgesic agents initiate their mode of action through direct binding at selective inhibitory receptor sites (Figure I-19). Figure 1-19. Summary of the different receptor sites at the dorsal horn related to inhibition and or excitation of incoming nociceptive afferent impulses Figure 1-19. Summary of the...

Limited access to the CNS

A2-receptors located in regions of the brain such as the nucleus tractus solitarius. Stimulation of these a2-receptors brings about a decrease in sympathetic outflow from the CNS, which in turn leads to decreases in peripheral vascular resistance and blood pressure.20,38 Bradycardia is also produced by clonidine as a result of a centrally induced facilitation of the vagus nerve and stimulation of cardiac prejunctional a2-receptors.39 These pharmacological actions have made clonidine quite...

Chemical Structure Of Oxytetracycline

R., and Ireland, D. S. Adv. Pharmacol. Chemother. 15 161, 1978. Values taken from Colazzi, J. L., and Klink, P. R. J. Pharm. Sci. 58 158, 1969. aValues taken from Brown, J. R., and Ireland, D. S. Adv. Pharmacol. Chemother. 15 161, 1978. Values taken from Colazzi, J. L., and Klink, P. R. J. Pharm. Sci. 58 158, 1969. for example, 7-dimethylamino, 7-chloro, and 6-methyl, have the opposite effect. Accordingly, the partition coefficient of chlortetracycline is...

Oxidation Involving Carbonnitrogen Systems

Metabolism of nitrogen functionalities e.g., amines, amides is important because such functional groups are found in many natural products e.g., morphine, cocaine, nicotine and in numerous important drugs e.g., phenothiazines, antihistamines, tricyclic antidepressants, j-adrenergic agents, sympathomimetic phenylethylamines, benzodiazepines .159 The following discussion divides nitrogen-containing compounds into three basic classes 1. Aliphatic primary, secondary, and tertiary and alicyclic...

The History Of Medicinal Chemistry

There is a long history of plants being used to treat various diseases. They figure in the records of early civilisations in Babylon, Egypt, India and China. The therapeutic properties of plants were described by the Ancient Greeks and by the Romans and are recorded in the writings of Hippocrates, Dioscorides, Pliny and Galenus. Some metals and metal salts were also used at this time. In the Middle Ages various 'Materia Medica and pharmacopeas brought together traditional uses of plants. The...

Antithyroid Drugs And Other Thyroid Inhibitors

A large number of compounds interfere either directly or indirectly with the synthesis, release, or action of thyroid hormones (Table 56-2). Inhibitors are classified into four categories (1) antithyroid drugs, which interfere directly with the synthesis of thyroid hormones (2) ionic inhibitors, which block the iodide transport mechanism (3) high concentrations of iodine itself, which decrease release of thyroid hormones and may also decrease hormone synthesis and (4) radioactive iodine, which...

Pathophysiological Events in Neuronal Network

What is happening at the neuronal network level when neurons transition from their normal firing pattern to the interictal condition and then to the ictal state Figure 5B depicts some of the physiologic features that accompany these changes. Now, rather than recording electrical activity from the surface of the brain, single electrodes are placed inside individual excitatory cortical neurons 1 and 2, thereby recording intracellular potentials. Much of our understanding of epilepsy mechanisms...

Cyp Benzylic Oxidation

The enzyme systems carrying out this biotransformation are referred to as mixed-function oxidases or monooxygen-ases.24,25 There is a large family that carry out the same basic chemical reactions. Their nomenclature is based on amino acid homology and is summarized in Table 3.2. There are four components to the name. CYP refers to the cytochrome system. This is followed by the Arabic number that specifies the cytochrome family (CYP1, CYP2, CYP3, etc.). Next is a capital letter that represents...

Medicinal Chemistry Of Sulfonylurea

See Table 20.1 for structural details of modified insulins. hUltralente (U) and Lente (L) insulins have been discontinued in the United States, supplanted by newer modified insulins and insulin mixtures. iv, intravenous OTC, over-the-counter rDNA, recombinant DNA sc, subcutaneous U, international activity units. See Table 20.1 for structural details of modified insulins. hUltralente (U) and Lente (L) insulins have been discontinued in the United States, supplanted by newer modified insulins and...

O Synthetic Cholinergic Blocking Agents

The solanaceous alkaloids are generally agreed to be potent parasympatholytics, but they have the undesirable property of producing a wide range of effects through their nonspecific blockade of autonomic functions. Efforts to use the antispasmodic effect of the alkaloids most often result in side effects such as dryness of the mouth and fluctuations in pulse rate. Therefore, synthesis of compounds possessing specific cholinolytic actions has been a very desirable field of study. Few...

O General Pathways Of Drug Metabolism

Drug metabolism reactions have been divided into two categories phase I (functionalization) and phase II (conjugation) reactions.1'7 Phase I, or functionalization reactions, include oxidative, reductive, and hydrolytic biotransformations (Table 3.1).8 The purpose of these reactions is to introduce a functional polar group(s) (e.g., OH, COOH, NH2, SH) into the xenobiotic molecule to produce a more water-soluble compound. This can be achieved by direct introduction of the functional group (e.g.,...

Neurotransmitter And Neuropeptide Systems Serotonergic System

Largely on the basis of the observation that most current effective antidepressants and antipsychotics target these systems, the monoaminergic systems (e.g., serotonin, norepinephrine, dopamine) have been extensively studied. Serotonin (5-HT) was given that name because of its activity as an endogenous vasoconstrictor in blood serum (Rapport et al. 1947). It was later acknowledged as being the same molecule (secretin) found in the intestinal mucosa and that is secreted by chromaffin cells...

Neuroanatomy Of The Dopamine System

The precursor for dopamine (DA), and all catecholamines, is the amino acid tyrosine. The rate-limiting step in DA synthesis is the conversion of tyrosine to L-dihydroxyphenylalanine (L-dopa) by the enzyme tyrosine hydroxylase. DA is then formed by decarboxylation of L dopa via the enzyme L-aromatic amino acid decarboxylase. DA neurotransmission is terminated through the actions of the dopamine transporter (DAT) (Jaber et al. 1997), although in some areas where the amount of DAT is low,...

Substituents Of Risperidone

A dibenzoxazepine derivative in use is loxapine succinate, f 1,4 oxazepine succinate (Daxolin). The structural relationship to the phenothiazine antipsychotics is apparent. Examples in this group are clothiapine, metiapine, zotepine, and others. They have electron-withdrawing groups at position 2, relatively close to the side-chain nitrogen atoms. Loxapine, an effective antipsychotic, blocks D2-type receptors and has side effects similar to those reported for the phenothiazines. Its...

Titanium Anticancer Drugs

After the discovery of the tumor-inhibiting properties of cis-diammine dichloro-platinum(II) (cisplatin) in 196912 and its routine use as a leading cytostatic drug since 1979,13 there has been increasing interest in the development of new anti-tumor metal agents including non-platinum metal complexes. Among these, two monomeric titanium(IV) complexes have qualified for clinical trials (Figure 7.1) TiIV(bzac)2(OEt)2 (budotitane) and Cp2TiIVCl2 (titanocene dichloride). Relevant reviews on...

Midazolam Log P 367 t12 2 h

Zolpidem Ambien, an imidazopyridine and eszopiclone Lunesta, a cyclopyrrolone are nonben-zodiazepines and have been introduced as short- and moderate-acting hypnotics, respectively. Zolpidem exhibits a high selectivity for the ai subunit of benzodiazepine-binding site on GABAA receptor complex, whereas es-zopiclone is a superagonist at BzRs with the subunit composition a1p2j2 and a1j2y3. Zolpidem has a rapid onset of action of 1.6 hours and good bioavailability 72 , mainly because it is...

Structure Activity Relationships of the Volatile General Anesthetics

The inhalation anesthetics in use today are nitrous oxide, halothane, isoflurane, desflurane, and sevoflurane. The chemical structures for these compounds and some of historical interest can be seen in Figure 22.1. While it is true that there is no single pharmacophore for the inhaled anesthetics, the chemical structure is related to the activity of the drug molecule. The first SAR studies conducted independently by Meyer and Overton in the 1880s showed a distinct positive correlation between...

O Antibiotics And Natural Products

A variety of the anticancer agents available today are derived from natural sources with several of these being obtained from microbial sources (antibiotics). Many of the antineo-plastic antibiotics are produced by the soil fungus Streptomyces. Both the antibiotic and natural product classes have multiple inhibitory effects on cell growth however, they primarily act to disrupt DNA function and cell division. There are several mechanisms by which these agents target DNA, including intercalation,...

Hydralazine Acetylation

The metabolism of the immunosuppressive drug azathio-prine Imuran to and 6-mercaptopurine is an example of hetero-aromatic nucleophilic substitution involving GSH.433-435 Interestingly, 6-mercaptopurine formed in this reaction appears to be responsible for azathioprine's immunosuppressive activity.436 Arene oxides and aliphatic epoxides or oxiranes represent a very important class of substrates that are conjugated and detoxified by GSH.437 The three-membered oxygen-containing ring in these...

Structureactivity Relationships

The structure-activity relationships (SARs) summary is shown in Figure 16.11. Comprehensive reviews of the SARs of a- and -agonists and antagonists33-35 covered their developments in the late 1980s. The parent structure with the features in common for many of the adrenergic drugs is -phenylethylamine. The manner in which -phenylethylamine is substituted on the meta- and para-positions of the aromatic ring, on the amino (R1), and on a-, (R2)-, and -positions of the ethylamine side chain...

Nonprotoplasmic Ergastic Cell Contents

Calcium Oxalate Many plants detoxify soluble oxalic acid as insoluble calcium salts. Calcium oxalate crystallizes in characteristic forms these shapes can be very important for diagnostic purposes Figures 7.12 and 7.13 . The exact crystallographic forms of these crystals are determined by measuring their angles. This is difficult and many technical and nontechnical terms are used to describe them. Calcium oxalate crystals are birefractive birefringent , which makes them visible in polarized...

Stereochemistry Of Cancer Drugs

In a lecture, held much later in Utrecht on May 16,1904, van't Hoff said the following Students, let me give you a recipe for making discoveries. In connexion with what has just been said about libraries, I might remark that they have always had a mind-deadening effect on me. When Wislicenus' paper on lactic add appeared and I was studying it in the Utrecht library, I therefore broke off my study half-way through, to go for a walk and it was during this walk, under the influence of the...

Quantitative Microscopy

In addition to measuring the size of cells and tissues with the eyepiece or stage micrometers, a number of other quantitative values are utilized for the microscopic evaluation of botanicals (predominantly leaves). These include palisade ratios, vein islet and stomatal numbers, and sto-matal index Palisade ratios. The palisade ratio is the average number of palisade cells that occur beneath an epidermal cell. The palisade ratio of many plants remains constant regardless of geographical location...

Oxidative Damage to Carbohydrates

The endogenous Maillard reaction, that is, the formation of Maillard reaction products in vivo, commonly known as the glycation reaction, is recognized today as one of many non-enzymatic modifications of proteins that not only contribute to the aging of the body's proteins, but may also have an important regulatory role in both physiological responses and pathological processes 118 . A major outcome of the studies on glycation was the recognition that oxidative reactions, and by inference,...

A1 Adrenergic Antagonists

Drugs that selectively block a1 adrenergic receptors without affecting a2 adrenergic receptors also are used in hypertension (Table 32-2). Prazosin (minipress), terazosin (Hytrin), and doxazosin (Cardura) are the agents approved in the U.S. for this indication. PHARMACOLOGICAL EFFECTS Initially, a1 adrenergic receptor antagonists reduce arteriolar resistance and increase venous capacitance this causes a sympathetically mediated reflex increase in heart rate and plasma renin activity. During...

Anatomical And Physiological Considerations Of The Gastrointestinal Tract

The GIT is a highly specialized region of the body whose primary functions involve the processes of secretion, digestion, and absorption. Since all nutrients needed by the body, with the exception of oxygen, must first be ingested orally, then processed by the GIT, and then made available for absorption into the bloodstream, the GIT represents a significant barrier and interface with the environment. The primary defense mechanisms employed by the gut to rid it of noxious or irritating materials...

Half Life of Detection and Cut Offs in Urine Drug Screening

Drug screening tests offer a fast and reliable way to demask a possible drug consumer. Various tests are available as individual tests for 12 drugs and medications as well as different combinations are offered which can be used in diverse circumstances, according to customer needs (Table V-4). They range from quick, competitive, stringent immunoassays to directly qualitative indications of drugs in urine. Depending on the time of abuse there is a large variability in half-life during which the...

Methods Of Vaccine Production

Vaccine production methods have varied greatly over the years and are best discussed according to a parallel chronological and sophistication approach. In this method, the normal pathogen is treated with a strong, denaturing disinfectant like formaldehyde or phenol. The process denatures the proteins and carbohydrates that are essential for the organism to live and infect a host, but if treated properly, the surface antigens are left intact. The process must be done carefully to control the...

Effects of Organ Size Blood Flow and Partition Coefficient on Distribution

A particular organ in the body may act as a site of distribution or as a site of both distribution and elimination. The relative importance of the various organs as storage or aExcerpted from Oie and Benet, Modern Pharmaceutics, 4th Edition. Figure 1 Process of drug absorption and distribution following administration of a single dose. The drug reaches the desired site of action either directly or via the general circulation. The drug may also reach other tissue sites or may be eliminated by...

The Endocrine System of Fish

To fully understand how these pollutants can affect fish at very low levels, it is necessary to outline very briefly how the endocrine system works. It is a control system of the body which responds to internal and external signals to maintain the body in a chemical equilibrium, to regulate sexual development and the seasonal reproductive cycles, and to evoke a stress response to external threats. At its core are the hypothalamus and pituitary, which respond to neural signals from the brain and...

Importance of Biopharmaceutics in the Overall Development Process

Biopharmaceutics is an integral component of the overall development cycle of a drug. Evaluation begins during the drug discovery process, proceeds through compound selection, preclinical efficacy and safety testing, formulation development, clinical efficacy studies, and postapproval stages. At each stage, biopharmaceuti-cal scientists interface with colleagues in multiple disciplines including discovery chemistry and biology, drug safety assessment, clinical development, pharmaceutical...

Brief Account Of The Role Of Chemistry In Cancer Chemotherapy

Chemistry has had varying roles in the discovery and development of anticancer drugs since the beginning of cancer therapies.13 In its early history, chemical modification of sulfur mustard gas led to the serendipitous discovery of the still clinically useful nitrogen mustards. Since those years, synthetic chemistry has been extensively used to modify drug leads, especially those of natural origin, and to solve the problem of the often scarce supply of natural products by developing...

O Antibacterial Sulfonamides

The sulfonamide antimicrobial drugs were the first effective chemotherapeutic agents that could be used systemically for the cure of bacterial infections in humans. Their introduction led to a sharp decline in the morbidity and mortality of infectious diseases. The rapid development of widespread resistance to the sulfonamides soon after their introduction and the increasing use of the broader-spectrum penicillins in the treatment of infectious disease diminished the usefulness of sulfonamides....

Common Comprehensions on Prescription Drug Abuse

The street value of a prescription drug is dependent on whether it is a brand or generic. Even abusers know that they get what they pay for when buying a brandname drug. Drugs that have a quick onset - immediate-release or injectable drugs -are more sought after, as well as those that have a greater intensity. The demand for drugs with a short duration of action is consistent with the rate hypothesis of reinforcement - the faster the drug enters the system, the quicker it causes the dopamine...

Ginsengasian Panax ginseng Ginsana G115 Korean red ginseng

Promoted to improve vitality and well-being 200 mg PO daily. Ginsana 2 caps PO daily or 1 cap PO bid. Ginsana Sport 1 cap PO daily. Preliminary evidence of efficacy for erectile dysfunction. Efficacy unclear for improving physical or psychomotor performance, diabetes, herpes simplex infections, cognitive or immune function. American College of Obstetrics and Gynecologists and North American Menopause Society recommend against use for postmenopausal hot flashes. Not by prescription. 2- - GINSENG...

Sar Of Benzodiazepines

Although the brain is undoubtedly the most wondrously complex organ, it is possible to distil the way it works into two opposing forces excitation and inhibition (depressing). Central nervous system (CNS) depressants are drugs that can be used to slow down or depress the functions of the CNS. Although many agents have the capacity to depress the function of the CNS, CNS depressants discussed in this chapter include only anxiolytics, sedative-hypnotics, and antipsychotics. There is some overlap...

Vasoactive substances

Substances released from many cells and tissues in the body, including the endothelium lining blood vessels, endocrine glands, and myocytes in the heart, may affect vascular smooth muscle tone. These substances may stimulate this muscle to cause vasoconstriction or inhibit it to cause vasodilation. As expected, vasoconstriction will increase TPR (and therefore MAP) and vasodilation will decrease TPR (and therefore MAP). Vasoconstrictors. Many substances produced in the human body cause...

Poorly Absorbed Sulfonamides

Sulfasalazine (azulfidine) is very poorly absorbed from the GI tract and is used in the therapy of ulcerative colitis and Crohn's disease (see Chapter 38). SULFONAMIDES FOR TOPICAL USE Sulfacetamide Sulfacetamide is the N1-acetyl-substituted derivative of sulfanilamide. Its aqueous solubility is 90 times that of sulfadiazine. This drug (isopto-cetamide, others) is employed extensively for ophthalmic infections. Very high aqueous concentrations are not irritating to the eye and are effective...

Factors Affecting Dissolution

Several physicochemical processes need to be considered along with the drug substance dissolution process to determine the overall dissolution rate of drugs from solid dosage forms under standardized conditions. The dissolution process for a solid dosage form (or a drug product) in solution starts with the wetting and the penetration of the dissolution medium into the solid formulation. It is generally followed by disintegration and or deaggregation into granules or fine particles. However,...

Selective NRI Safety and Tolerability

The side-effect profiles of reboxetine, atomoxetine, and viloxazine can be attributed to the unwanted effects of norepinephrine, as activity at other receptors is limited. The concept of selectivity can thus be a bit deceiving. While an agent such as reboxetine is selective for the neurotransmitter norepinephrine, its activity is nonse-lective in terms of distribution, contributing to effects not only in the brain but in the body as well (Table 3). In the limbic system, the stimulation of...

Pyridine and piperidine alkaloids

Alkaloids, e.g. piperine, coniine, trigonelline, pilocarpine, nicotine and sparteine, possess a pyridine or modified pyridine heterocyclic ring system (e.g. piperidine ring). Piperine Piperine, molecular formula Ci7H19NO3, a component of black pepper (Piper nigrum), has been used in various traditional medicine preparations, and also as an insecticide. Piperine has various effects on human drug metabolizing enzymes, and is marketed under the brand name, Bioperine , as an adjunct for increasing...

Drug Receptor Interactions

Although the Hansch reasoning does apply to the interaction of a drug with its receptor, many of the factors that are considered relate to the substance crossing barriers and entering different cellular phases. When we consider a drug interacting with a receptor or an enzyme system, there are a number of physico-chemical features that must be taken into account. A receptor or an enzyme system comprises a highly structured chiral environment dominated not just by the pockets created by the...

Mechanism Of Action Of Tricyclic Antidepressants

The termination of action of biogenic amines norepinephrine (NE) and serotonin (5-HT) is determined by reuptake into the presynaptic terminal. Drugs that block reuptake, such as tricyclic antidepressants, increase the efficacy of those transmitters by allowing them to remain in the synaptic cleft and activate the receptors longer (Figure I-51). It should be noted that although the exact mechanism of action of TCAs as analgesics is not known, there appears to be a close relationship between the...

Essentials For Human Physiology

AHFS Drug Information 2000, American Society of Health-System Pharmacists, Bethesda, MD, 2000. 2. Bell, D.R., Core Concepts in Physiology, Lippincott-Raven Publishers, Philadelphia, 1998. 3. Costanzo, L., Physiology, W.B. Saunders, Philadelphia, 1998. 4. Guyton, A.C. and Hall, J.E., Textbook of Medical Physiology, 10th ed., W.B. Saunders, Philadelphia, 2000. 5. Hunt, M.L., Jr., Training Manual for Intravenous Admixture Personnel, 5th ed., Baxter Healthcare Corp., 1995. 6. Lombard, J.H. and...

Coanalgesics For Chronic Pain

Coanalgesics are a varied group of medications that can provide additive pain relief when they are added to nonsteroidal anti-inflammatory drugs (NSAIDs) or opioids (American Pain Society APS , 2008). They can have independent analgesic activity for some painful complaints, and they can counteract select adverse effects of analgesics (APS, 2008). This group of medications was developed to treat a wide variety of conditions, such as seizures or muscle spasms, and was originally intended for...

Hypolipidemic Hypocholesterolemic Drugs

The fact that even young men can develop atherosclerosis was reported following autopsies of German soldiers during World War I. However, it was a U.S. Armed Forces Institute of Pathology report toward the end of the Korean War (Enos et al., 1953) showing that young men (average age 22) had evidence of coronary heart disease (CHD) that made the medical profession take note of the epidemic that was CHD. The problem is still extensive in spite of considerable, but slow, progress since the 1950s....

ALIS An Affinity Selection Mass Spectrometry System based on Continuous SEC

The schematic shown in Fig. 3.1 describes an optimized, integrated SEC-RPC-MS-based affinity selection platform developed at NeoGenesis, dubbed the Fig. 3.1 Schematic of ALIS, an automated ligand identification system that uses continuous size-exclusion chromatography for the study of protein-ligand interactions. Fig. 3.1 Schematic of ALIS, an automated ligand identification system that uses continuous size-exclusion chromatography for the study of protein-ligand interactions. Automated Ligand...

Advantages and Limitations of Microdialysis

Since its first applications, microdialysis has become increasingly popular to study brain function. The use of alternative in vivo procedures such as push-pull perfusion or voltammetry has remained constant or even declined during last years. A comparison between microdialysis and voltammetry reveals that microdialysis is applicable to most types of small molecules whereas the use of voltammetry is limited to easily oxidizable compounds such as catecholamines and serotonin. Moreover,...

Chances Stopped Flow Technique Revolutionized the Investigation of Moderately Fast Reactions

To eliminate the need for large volumes of reactants and to increase the versatility of measurement, Chance (1943) invented the stopped-flow apparatus by adding a third stopping syringe to receive the mixed reactant solutions after passage through the mixer and observation cuvette (see Fig. 10.4). The two reactant syringes are attached to a pneumatic piston that is driven by compressed nitrogen gas. As the third syringe fills, its retreating plunger contacts an electronic switch, stopping the...

Parenteral Vasodilators

The failing left ventricle is characterized by depression of myocardial contractility and increased sensitivity to alterations of left ventricular afterload. This latter attribute of the failing ventricle is manifest by a greater proportional reduction of stroke volume as the impedance to ejection is increased. Conversely, afterload reduction in this setting can be associated with substantial increases in stroke volume. This increased afterload dependence underlies the beneficial effects of...

Limitations Of Current Cancer Therapies

Today, surgery, radiotherapy, and chemotherapy, i.e. 'scalpel, ray, and pill', remain the standard tumor therapies. Novel therapies like gene therapy or immunotherapy are only administered in the setting of experimental studies. In addition, outside 'school' medicine, a variety of 'alternative' treatments are sought by patients and their families who do not have full confidence in standard therapies. This scepticism is, unfortunately, not entirely unfounded. With current therapies, between 30...

Topical Tricyclic Antidepressants

Few classes of drugs are more extensively used in the management of chronic pain conditions than the tricyclic antidepressants (TCAs). Substantial and convincing evidence supports their use in a variety of pain conditions including neuropathic pain and the pain associated with fibromyalgia. Their use is so common that it is now normal for them to be initiated by General Practitioners. The pain relief that may be apparent is independent of their antidepressant effects but any mood improvement...

Selection Of Antihypertensive Drugs In Individual Patients

Choice of an antihypertensive drug should be driven by likely benefit in an individual patient, taking into account concomitant diseases such as diabetes mellitus, problematic adverse effects of specific drugs, and cost. Consensus guidelines recommend diuretics as preferred initial therapy for most patients with uncomplicated stage 1 hypertension who are unresponsive to nonpharmacological measures. Patients are also commonly treated with other drugs p receptor antagonists, ACE inhibitors A...

Neuropathic Pain Scale

Thie NPS (Exhibit 15.1) was developed as a result of two research protocols in which pain descriptors were assessed for four different pain conditions PHN, CRPS, PDN, and traumatic peripheral nerve injury. A second, more diverse group of patients being treated with either lidocaine or phentolamine infusions used the scale to rate their pain. Interestingly, the second protocol outcome identified a positive response for pain that was described as unpleasant or deep. This finding led researchers...

The Neurogenic Inflammation Theory Of Migraines

This theory suggests that migraine headaches occur as a result of an abnormal firing of meningeal nociceptors at the TGVS. Activation of trigeminal neurons releases vasoac-tive peptides including calcitonin gene-related peptide (CGRP, a vasodilator peptide), substance P, and neurokinin A (both play an important role in pain transmission as well as activation of immune responses and neurogenic inflammation) onto dural tissue where these peptides produce a local response known as neurogenic...

Pharmacotherapy Of Gout

Gout results from the precipitation of urate crystals in the tissues and the subsequent inflammatory response. Acute gout usually causes an exquisitely painful distal monoarthritis, but it also can cause joint destruction, subcutaneous deposits (tophi), and renal calculi and damage. Gout affects -0.5-1 of the population of Western countries. The pathophysiology of gout is understood poorly. While a prerequisite, hyperuricemia does not inevitably lead to gout. Uric acid, the end product of...

Short Form McGill Pain Questionnaire2 SFMPQ2

In the original McGill Pain Questionnaire used to assess pain in chronic pain patients, there is a list of 15 verbal descriptors rated on a 4-point scale, a visual analog scale for pain intensity, and verbal rating scales. The original scale established reliability and validity for measuring pain in chronic pain conditions. Although some chronic pain conditions are neuropathic, a tool that can distinguish both the pain of a chronic no-ciceptive condition and neuropathic pain is considered...

Epidemiology of nonspecific neck pain

Epidemiological studies of neck pain are based on questionnaires and surveys, which may overestimate the frequency of the condition. Nevertheless, it is clear that nonspecific neck pain including whiplash places a heavy burden on individuals, employers, and healthcare services. About two-thirds of the population will experience neck pain at some time in their lives 7, 8 , with the condition being most common in middle age, and in women 9 . The reported prevalence of neck pain varies widely...

Tests For Extraneous Agents In Viral Vaccines For Human

In those tests that require prior neutralisation of the virus, use specific antibodies of non-human, non-simian origin if the virus has been propagated in avian tissues, the antibodies must also be of non-avian origin. To prepare antiserum, use an immunising antigen produced in cell culture from a species different from that used for the production of the vaccine and free from extraneous agents. Where the use of SPF eggs is prescribed, the eggs are obtained from a flock free from specified...

Neurochemistry of Mental Disease

Can abnormalities in the steady state of biogenic amines (NE, DA, 5-HT) and other neurotransmitters of the CNS be causative factors in mental diseases such as schizophrenia, endogenous depression, and manic behavior Only 50 years ago arguments in favor of such a notion would have elicited, at best, benign smiles of amusement from an audience of psychiatrists. It is interesting that some experiments in the 1880s had suggested a possibility of chemical factors affecting the pathology of...