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Codeine Sulfate : Discussion About Analytic Pharmacology And Nonclinical Toxicology

codeine sulfate

Mechanism of Action:

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Codeine Sulfate is an opioid analgesic, accompanying to morphine, but with beneath almighty analgesic properties. Codeine is careful for the mu receptor, but with a abundant weaker affection than morphine. The analgesic backdrop of codeine accept been speculated to appear from its about-face to morphine, although the exact apparatus of analgesic action charcoal unknown.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Effects on the Central Nervous Arrangement (CNS) :

Analytical pharmacology and nonclinical toxicology of codeine sulfate

The arch ameliorative action of Codeine Sulfate is analgesia. Although the absolute apparatus of the analgesic action is unknown, specific CNS analgesic receptors and autogenous compounds with morphine-like action accept been articular throughout the academician and analgesic bond and are acceptable to comedy a role in the announcement and acumen of analgesic effects. Some added CNS furnishings of codeine accommodate anxiolysis, euphoria, and animosity of relaxation/relax condition. Codeine Sulfate is responsible for respiratory depression, in allotment by a absolute aftereffect on the brainstem respiratory centers. Codeine Sulfate and added accompanying opioids abase the ahem reflex by absolute aftereffect on the ahem centermost in the medulla. Codeine Sulfate may additionally account miosis.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Effects on the Gastrointestinal Amplitude (GIT) and on Added Smooth Muscle :

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Gastric, biliary and pancreatic secretions may be decreased by codeine. Codeine additionally causes a abridgement in action and is associated with an access in accent in the antrum of the abdomen and duodenum. Digestion of aliment in the baby civil is delayed and active contractions are decreased. Active peristaltic after-effects in the colon are decreased, while accent is added to the point of spasm. The end aftereffect may be constipation. Codeine can account a credible access in biliary amplitude burden as a aftereffect of the access of the sphincter of Oddi. Codeine may additionally account spasms of the sphincter of the urinary bladder.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Effects on the Cardiovascular Arrangement :

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Codeine produces borderline vasodilation which may aftereffect in orthostatic hypotension and fainting. Absolution of histamine can occur, which may comedy a role in opioid-induced hypotension. Manifestations of histamine absolution and/or borderline vasodilation may accommodate pruritus, flushing, red eyes, and sweating.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Endocrine Arrangement :

Opioid agonists such as Codeine Sulfate accept been credible to accept a array of furnishings on the beard of hormones. Opioids arrest the beard of ACTH, cortisol, and luteinizing hormone (LH) in humans. They additionally activate prolactin, advance hormone (GH) secretion, and pancreatic beard of insulin and glucagons in bodies and added species, rats and dogs. Thyroid aesthetic hormone (TSH) has been credible to be both inhibited and angry by opioids.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Immune Arrangement :

Codeine has been credible to accept a array of furnishings on apparatus of the allowed arrangement in in vitro and beastly models. The analytic acceptation of these allegation is unknown.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Pharmacodynamics

Codeine concentrations do not associate with academician assimilation or abatement of pain.

The minimum able assimilation varies broadly and is afflicted by a array of factors, including the admeasurement of antecedent opioid use, age and accepted medical condition. Able doses in advanced patients may be decidedly college than in opioid-naive patients.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Pharmacokinetics :

Absorption

Codeine is captivated from the gastrointestinal amplitude with best claret assimilation occurring 60 account column administration.

Food Furnishings/Effects

When 60 mg of the Codeine Sulfate was administered 30 account afterwards ingesting a aerial fat/high calorie meal, there was no cogent change in the amount and admeasurement of assimilation of codeine.

Steady-state –

Administration of 15 mg of the Codeine Sulfate every/each four hours for 5 canicule resulted in steady-state concentrations of codeine, morphine, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) aural 48 hours.

Distribution :

Codeine has been appear to accept an credible aggregate of administration of about 3-6 L/kg, advertence all-encompassing administration of the biologic into tissues. Codeine has low claret protein bounden with about 7-25% of codeine apprenticed to claret proteins.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Metabolism :

About 70-80% of the administered dosage of codeine is metabolized by alliance with glucuronic acerbic to codeine-6-glucuronide (C6G) and via O-demethylation to morphine (about 5-10%) and N-demethylation to norcodeine (about 10%) respectively/separately. UDP-glucuronosyltransferase (UGT) 2B7 with 2B4 are the above enzymes mediating glucurodination of codeine to C6G. Cytochrome P450 2D6 is the above agitator amenable for about-face of codeine to morphine and P450 3A4 is the above agitator mediating about-face of codeine to norcodeine. Morphine and norcodeine are added metabolized by alliance with the glucuronic acid. The glucuronide metabolites of the morphine are morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G). Morphine and M6G are accepted to accept analgesic action in humans. The analgesic action of C6G in bodies is unknown. Norcodeine and M3G are about not advised to acquire analgesic properties.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Elimination/Excretion :

Approximately 90% of the absolute dosage of codeine is excreted through the kidneys, of which about 10% is banausic codeine. Claret half-lives of codeine and its metabolites accept been appear to be about 3 hours.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Nonclinical Toxicology

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Carcinogenesis, Mutagenesis, Impairment of Fertility :

Carcinogenesis: Two year carcinogenicity studies accept been conducted in F344/N rats and B6C3F1 mice. There was no affirmation of carcinogenicity in macho and changeable rats, respectively, at comestible doses up to 70 and 80 mg/kg/day of codeine (approximately 2 times the best recommended circadian dosage of 360 mg/day for adults on a mg/m2 basis) for two years. Similiarly there was no affirmation of carcinogenicity action in macho and changeable mice at comestible doses up to 400 mg/kg/day of codeine (approximately 5 times the best recommended circadian dosage of 360 mg/day for adults on a mg/m2 basis) for two years.

Mutagenesis: Codeine wasn’t mutatgenic in the in- vitro bacterial about-face alteration appraisal or clastogenic in the in vitro Chinese hamster ovary corpuscle chromosome abnormality assay.

Impairment of fertility: No beastly studies were conducted to appraise the aftereffect of codeine on macho or changeable fertility.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

Reproduction And Adorning Toxicology –

Studies on the changeable and adorning furnishings of codeine accept been appear in the appear abstract in hamsters, rats, mice and rabbits.

A abstraction in hamsters administered 150 mg/kg bid of codeine (PO; about 7 times the best recommended circadian dosage of 360 mg/day for adults on a mg/m2 basis) appear the development of cranial malformations/deformities (i.e., meningoencephalocele) in several of the fetuses examined; as able-bodied as the ascertainment of increases in the allotment of resorptions per clutter examined. Doses of 50 and 150 mg/kg, bid resulted in fetotoxicity as approved by decreased fetal anatomy weight. In an beforehand abstraction in hamsters, doses of 73-360 mg/kg akin (PO; about 2-8 times the best recommended circadian dosage of 360 mg/day for adults on a mg/m2 basis), reportedly producing the cranioschisis in all of the fetuses examined.

In studies in rats, doses at the 120 mg/kg akin (PO; about 3 times the best recommended circadian dosage of 360 mg/day for adults on a mg/m2 basis), in the baneful ambit for the developed animal, were associated with an access in antecedent absorption at the time of implantation.

In abundant mice, a distinct 100 mg/kg dosage (SC; about 1.4 times the recommended circadian dosage of 360 mg/day for adults on a mg/mg2 basis) reportedly resulted in delayed ossification in the offspring.

No teratogenic furnishings were empiric in rabbits administered up to 30 mg/kg (approximately 2 times the best recommended circadian dosage of 360 mg/day for adults on a mg/m2 basis) of codeine during organogenesis.

Analytical pharmacology and nonclinical toxicology of codeine sulfate

About Dr. Md. Kafil - Uddin Sarker Akash

Short Biography Of The Hon’ble Chairman : Dr. Md. Kafil – Uddin Sarker Akash, Hon’ble Chairman, Bangladesh Preventive Welfare Society of Suicide-Addiction-Narcotics & Pollution(BPWS of SANP), was born on December 31 (Thirty One), 1982 in the Village : Nilam Kharida Sadra, P.O- Vayerhat, P.S- Kaunia, District- Rangpur, Country- Bangladesh. He is the son of Md. Nurul Islam and Most. Noorjahan Begum. Having obtained Bachelor of Medicine and Bachelor of Surgery (M.B.B.S) under University of Rajshahi, Bangladesh and he was enrolled as a Registered Doctor from “ Bangladesh Medical & Dental Council” -(BM&DC) ; And achieved Post-Graduation Degree on Forensic Medicine (D.F.M) ; Under Bangabandhu Sheikh Mujib Medical University(BSMMU), Bangladesh and Also achieved (M.C.P.S) Membership, From Bangladesh College of Physician & Surgeons -(B.C.P.S). Currently, he is Fellow in Phd Research Program at Institute of Biological Science under University of Rajshahi, Bangladesh. He practiced as Reputed Physician and Work as a Autopsy Surgeon through conducted several Post-mortem Examinations and delivered huge expert Medico-Legal Opinion under Court of Law to aid for Administration of Justice. In additionally, he participate in many short and long time training program, Scientific Seminar, Symposium and Obtained many of the Training Certificates. He also conducted and taken Lecture Class in different Medical Colleges of Bangladesh for a longer period of time. Thus, he get opportunity to build intimacy and make friendly relationship among with the huge students and try to understand psychology of different level students. He also build and make intimacy with the huge General Peoples through visited on different region locally, internationally and See how to suffer the peoples due to anxiety, stress, depression, addiction, abuse and dependence, effects of different pollution, contamination and intoxication, harmful effects due to destruction of nature and natural environment, effects of climate change and suffer different health hazards for that reasons etc. Thus, he inspire and encouraged for doing something of the human being, that would be ensure welfare need of the world peoples.

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