The prodrug concept was first proposed in 1958 as a way to temporarily modify drugs' physicochemical properties to improve their usefulness and decrease toxicity. Prodrugs are converted to the active drug within the body through enzymatic or non-enzymatic reactions. This allows for improved solubility, delivery, stability, and decreased adverse effects. Ideal prodrugs are inactive or less active than the parent drug, are cleaved in vivo to release the parent drug, and produce non-toxic metabolic fragments. Common prodrug modifications include esterification of carboxylic acids and alcohols as well as derivatization of carbonyl groups. Successful prodrugs have been developed to improve patient acceptance, reduce gastric irritation,
THE PRODRUG DESIGNING FOR NEW SELECTION AND FORMULATION OF DRUG COMPATIBLE WITH API I.E. ACTIVE PHARMACUTICAL INGREDIENT, AND ITS EFFECT WHICH SHOULD BE 0. THE DRUG COMBINED WITH API AND AVILABLE IN MARKET AND DRUGS NEED TO BE COMBINE ARE ALSO DISCUSSED WITH ITS STRUCTURE AND SAR, AND COVERED AS PER THE SYLLABUS OF PCI.
THE PRODRUG DESIGNING FOR NEW SELECTION AND FORMULATION OF DRUG COMPATIBLE WITH API I.E. ACTIVE PHARMACUTICAL INGREDIENT, AND ITS EFFECT WHICH SHOULD BE 0. THE DRUG COMBINED WITH API AND AVILABLE IN MARKET AND DRUGS NEED TO BE COMBINE ARE ALSO DISCUSSED WITH ITS STRUCTURE AND SAR, AND COVERED AS PER THE SYLLABUS OF PCI.
Sythesis of heterocyclic drugs ketoconazole and metronidazoleandhra university
A Heterocyclic compounds are those which has atoms of at least two different elements as members of its ring.
Heterocyclic chemistry is a branch of organic chemistry dealing with the synthesis, properties, and applications of these heterocycles.
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
Macrolides are a class of antibiotics derived from Saccharopolyspora erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.
Sythesis of heterocyclic drugs ketoconazole and metronidazoleandhra university
A Heterocyclic compounds are those which has atoms of at least two different elements as members of its ring.
Heterocyclic chemistry is a branch of organic chemistry dealing with the synthesis, properties, and applications of these heterocycles.
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
Macrolides are a class of antibiotics derived from Saccharopolyspora erythraea (originally called Streptomyces erythreus), a type of soil-borne bacteria.
Basic concepts of Prodrug & their application in pharmacy fieldsSHUVAM SAR
Definition of prodrugs along with their uses in pharmacy have been discusses here in brief. Also includes the basic objectives of their formulation with examples.
Prodrugs an approach to solve problems related to admeJyotsna Patil
prodrugs an approach to overcome problems related to ADME, for MPharm students
sub- modern pharmaceutical and medicinal chemistry
branch- quality assurance
Commonly known as its anionic form shikimate, is a cyclohexene, a cyclitol and a cyclohexanecarboxylic acid.
It is an important biochemical metabolite in plants and microorganisms.
Its name comes from the Japanese flower shikimi the Japanese star anise, Illicium anisatum), from which it was first isolated in 1885 by Johan Fredrik Eykman.
The elucidation of its structure was made nearly 50 years later.
Shikimic acid is also the glycoside part of some hydrolysable tannins.
The shikimate pathway is a seven step metabolic route used by bacteria, fungi, algae, parasites, and plants for the biosynthesis of aromatic amino acids (phenylalanine, tyrosine, and tryptophan).
This pathway is not found in animals; therefore, phenylalanine and tryptophan represent essential amino acids that must be obtained from the animal's diet
Animals can synthesize tyrosine from phenylalanine, and therefore is not an essential amino acid except for individuals unable to hydroxylate phenylalanine to tyrosine).
1. Measurement of Bioavailability:
Direct and indirect methods may be used to assess drug bioavailability. The in-vivo bioavailability of a drug product is demonstrated by the rate and extent of drug absorption, as determined by comparison of measured parameters, e.g., concentration of the active drug ingredient in the blood, cumulative urinary excretion rates, or pharmacological effects.
For drug products that are not intended to be absorbed into the bloodstream, bioavailability may be assessed by measurements intended to reflect the rate and extent to which the active ingredient or active moiety becomes available at the site of action.
The design of the bioavailability study depends on the objectives of the study, the ability to analyze the drug (and metabolites) in biological fluids, the pharmacodynamics of the drug substance, the route of drug administration, and the nature of the drug product.
Pharmacokinetic and/or pharmacodynamic parameters as well as clinical observations and in-vitro studies may be used to determine drug bioavailability from a drug product.
1.1. Pharmacokinetic methods:
These are very widely used and based upon the assumption that the pharmacokinetic profile reflects the therapeutic effectiveness of a drug. Thus these are indirect methods. The two major pharmacokinetic methods are:
The major pharmacokinetic methods are:
Plasma / blood level time profile.
o Time for peak plasma (blood) concentration (t max)
o Peak plasma drug concentration (Cmax)
o Area under the plasma drug concentration–time curve (AUC)
Urinary excretion studies.
o Cumulative amount of drug excreted in the urine (Du)
o Rate of drug excretion in the urine (dDu/dt)
o Time for maximum urinary excretion (t)
C. Other biological fluids
1.2. Pharmacodynamic methods:
IT involves direct measurement of drug effect on a (patho) physiological process as a function of time. Disadvantages of it may be high variability, difficult to measure, limited choices, less reliable, more subjective, drug response influenced by several physiological & environmental factors.
They involve determination of bioavailability from:
Acute pharmacological response.
Therapeutic response.
1.3. In-vitro dissolution studies
Closed compartment apparatus
Open compartment apparatus
Dialysis systems.
1.4. Clinical observations
Well-controlled clinical trials
Chemical preservatives for semisolids must be carefully evaluated for their stability with regard to the other components of the formulation as well as to the container. Plastic containers may absorb the preservative and thereby decrease the quantity available for inhibiting or destroying the microorganism’s responsible for spoilage. Some preservatives may sting or irritate the mucous tissues of the eye or nasal passages. Methylparabens and propylparabens tend to be more irritating when applied in the nose than quaternary ammonium compounds or the phenylmercuric salts. Boric acid may be used in the ophthalmic preparations, but is omitted from products to be used in the nose because of possible toxic effects if absorbed in large quantities.
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
New Drug Discovery and Development .....NEHA GUPTA
The "New Drug Discovery and Development" process involves the identification, design, testing, and manufacturing of novel pharmaceutical compounds with the aim of introducing new and improved treatments for various medical conditions. This comprehensive endeavor encompasses various stages, including target identification, preclinical studies, clinical trials, regulatory approval, and post-market surveillance. It involves multidisciplinary collaboration among scientists, researchers, clinicians, regulatory experts, and pharmaceutical companies to bring innovative therapies to market and address unmet medical needs.
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
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New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
2. The Prodrug Concept
The prodrug concept was first proposed by Albert in 1958.
Albert and his co-workers described prodrugs as pharmacologically inactive chemical derivatives that could be used to alter the physicochemical properties of drugs, in a temporary manner, to increase their usefulness and/or to decrease associated toxicity.
They have also been called ‘latentiated drugs’, ‘bioreversible derivatives’, and ‘congeners’.
Ideally, the prodrug is converted to the original drug as soon as the derivative reaches the site of action, followed by rapid elimination of the released derivatizing group without causing side effects in the process.
3.
4.
5.
6. Applications Of Prodrug
Prodrugs are converted into the active drug within the body through enzymatic or non-enzymatic reactions. The various applications of prodrug approach are;
1. Improved physicochemical properties (e.g., better solubility in the intended formulation)
2. Enhanced delivery characteristics and/or therapeutic value of the drug
3. To improve drug penetration through biological membranes
4. To increase site specificity of the drug
5. To improve the drug’s stability and solubility
6. To increase duration of pharmacological activity
7. To decrease the drug’s toxicity and adverse effects
8. To improve patient acceptance.
7. Ideal Requirements of Prodrugs
1. The prodrug is inactive or less active than the parent compound
2. The linkage between the drug and the carrier must be cleaved in vivo
3. The carrier molecule released in vivo must be non-toxic
4. The metabolic fragments of carrier molecule, apart from the drug should be non-toxic
8. Classification of Prodrugs
1. Carboxylic acids and alcohols.
Prodrugs of carboxylic acid and alcohol functionalities can be prepared by conversion to an ester.
The ester can be easily hydrolysed by esterase enzymes present in plasma and other tissues to give active drug.
Enzymes: ester hydrolase, lipase, cholesterol esterase, acetylcholinesterase, carboxypeptidase
9. Carboxylic acids and alcohols (continued)...
Ex: Pivampicillin, talampicillin and bacampicillin are prodrugs of ampicillin.
The absorption of these prodrugs is nearly complete (98-99%) whereas that of ampicillin is < 50%.
Enalapril, the most widely prescribed ACE inhibitor, is the ethyl ester prodrug of the active diacid, enalaprilat.
Enalaprilat is poorly absorbed from the gastrointestinal tract (< 10%), but absorption of the prodrug enalapril is greatly improved (60%).
10. 2. Amines.
Due to high chemical stability of amide linkage and lack of amidase enzymes, amines are not derivatised to amide prodrugs.
A more common approach has been to utilize mannich bases as a prodrug form of the amines.
11. 3. Azo Linkage
Amines are derivatised to azolinkage prodrugs.
Ex: Prontosil
12. 4. Carbonyl compounds
Carbonyl compounds such as aldehydes and ketones are converted to prodrugs.
These have generally involved derivatives in which the sp2 hybridized carbonyl carbon is converted to an sp3 hybridised carbon attached to two heteroatoms such as oxygen, nitrogen, or sulfur.
Ex: Methenamine releases HCHO in the urine, which acts as an antibacterial agent.
13. Developments of Prodrugs
1. To improve patient acceptance:
Clindamycin has bitter taste. It was found that by increasing the chain-length of 2-acylesters of clindamycin, the taste improved from bitter to non-bitter taste (phosphate ester).
2. To reduce gastric irritation:
Several drugs (NSAIDS, nicotinic acid, kanamycin, diethylstilboestrol) cause irritation and damage to gastric mucosa.
These problems of drugs can be overcome by changing to prodrugs.
Ex. : Salicylic acid to aspirin, nicotinic acid to nicotinic acid hydrazide
14. Developments of Prodrugs (continued)…
3. To improve chemical stability:
Several drugs may decompose during their shelf life or in the GIT when used orally.
The prodrug approach of such drugs is a good technique to improve stability.
Ex. : Azacytidine in aqueous solution is readily hydrolyzed but its bisulphite prodrug is stable.
4. Prodrugs for increased water solubility:
Prednisolone and methylprednisolone are poorly water-soluble corticosteroid drugs.
Prednisolone phosphate is a water-soluble prodrug of prednisolone that is activated in vivo by phosphatases.
15. Developments of Prodrugs (continued)…
5. To decrease drug’s toxicity and adverse effects:
Dipivaloylepinephrine prodrug instead of epinephrine to treat glaucoma.
Esterification of aspirin greatly suppresses gastric uterogenic activity.
6. To improve membrane transport:
Barbiturates are weakly acidic in nature and are converted to the corresponding sodium salt. The sodium salt is extensively employed for intravenous anaesthetic properties.
Dopamine used for the treatment of Parkinson’s disease can be improved by administering its prodrug Levo-DOPA.
16. Developments of Prodrugs (continued)…
7. Prolonged Activity:
Nordazepam, an anxiolytic loses activity too quickly due to metabolism and excretion.
A prodrug introduced to improve the retention characteristics is (diazepum).
8. Tissue specific prodrug design:
The site-specific drug delivery can be achieved by the tissue activation, which is the result of an enzyme unique to the tissue or present in higher concentration.
Dexamethasone is absorbed efficiently in intestinal tract and as such do not reach colon area for treatment.
when prodrugs dexamethasone-21-β-glucoside were used they were absorbed in colon more efficiently compared to their parent drugs.