The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
Pharmacology: Pharmacodynamics: Nebido 1000mg/4 ml undecanoate is an ester of the naturally occurring androgen, Nebido 1000mg/4 ml. The active form, Nebido 1000mg/4 ml, is formed by cleavage of the side chain.
Nebido 1000mg/4 ml is the most important androgen of the male, mainly synthesized in the testicles, and to a small extent in the adrenal cortex.
Nebido 1000mg/4 ml is responsible for the expression of masculine characteristics during fetal, early childhood, and pubertal development and thereafter for maintaining the masculine phenotype and androgen-dependent functions (eg, spermatogenesis, accessory sexual glands). It also performs functions eg, in the skin, muscles, skeleton, kidney, liver, bone marrow and CNS.
Dependent on the target organ, the spectrum of activities of Nebido 1000mg/4 ml is mainly androgenic (eg, prostate, seminal vesicles, epididymis) or protein-anabolic (muscle, bone, hematopoiesis, kidney, liver).
The effects of Nebido 1000mg/4 ml in some organs arise after peripheral conversion of Nebido 1000mg/4 ml to estradiol, which then binds to estrogen receptors in the target cell nucleus eg, the pituitary, fat, brain, bone, and testicular Leydig cells.
Pharmacokinetics:Absorption: Nebido 1000mg/4 ml is an IM administered depot preparation of Nebido 1000mg/4 ml undecanoate and thus circumvents the first-pass effect. Following IM injection of Nebido 1000mg/4 ml undecanoate as an oily solution, the compound is gradually released from the depot and is almost completely cleaved by serum esterases into Nebido 1000mg/4 ml and undecanoic acid. An increase in serum levels of Nebido 1000mg/4 ml above basal values may be seen 1 day after administration.
Steady-State Conditions: After the 1st IM injection of Nebido 1000mg/4 ml undecanoate 1000 mg to hypogonadal men, mean Cmax values of 38 nmol/L (11 ng/mL) were obtained after 7 days. The 2nd dose was administered 6 weeks after the 1st injection and maximum Nebido 1000mg/4 ml concentrations of about 50 nmol/L (15 ng/mL) were reached. A constant dosing interval of 10 weeks was maintained during the following 3 administrations and steady-state conditions were achieved between the 3rd and the 5th administration. Mean Cmax and Cmin values of Nebido 1000mg/4 ml at steady state were about 37 (11 ng/mL) and 16 nmol/L (5 ng/mL), respectively. The median intra- and inter-individual variability (coefficient of variation, %) of Cmin values was 22% (range: 9-28%) and 34% (range: 25-48%), respectively.
Distribution: In serum of men, about 98% of the circulating Nebido 1000mg/4 ml is bound to sex hormone binding globulin (SHBG) and albumin. Only the free fraction of Nebido 1000mg/4 ml is considered as biologically active. Following IV infusion of Nebido 1000mg/4 ml to elderly men, the elimination half-life of Nebido 1000mg/4 ml was approximately 1 hr and an apparent volume of distribution of about 1 L/kg was determined.
Metabolism: Nebido 1000mg/4 ml which is generated by ester cleavage from Nebido 1000mg/4 ml undecanoate is metabolized and excreted the same way as endogenous Nebido 1000mg/4 ml. The undecanoic acid is metabolized by β-oxidation in the same way as other aliphatic carboxylic acids. The major active metabolites of Nebido 1000mg/4 ml are estradiol and dihydrotestosterone.
Elimination: Nebido 1000mg/4 ml undergoes extensive hepatic and extrahepatic metabolism. After the administration of radiolabeled Nebido 1000mg/4 ml, about 90% of the radioactivity appears in the urine as glucuronic and sulfuric acid conjugates and 6% appears in the feces after undergoing enterohepatic circulation. Urinary medicinal products include androsterone and etiocholanolone. Following IM administration of this depot formulation the release rate is characterized by a half-life of 90±40 days.
Toxicology:Preclinical Safety Data: Toxicological studies have not revealed other effects than those which can be explained based on the hormone profile of Nebido 1000mg/4 ml.
Nebido 1000mg/4 ml has been found to be nonmutagenic in vitro using the reverse mutation model (Ames test) or hamster ovary cells. A relationship between androgen treatment and certain cancers has been found in studies on laboratory animals. Experimental data in rats have shown increased incidences of prostate cancer after treatment with Nebido 1000mg/4 ml.
Sex hormones are known to facilitate the development of certain tumors induced by known carcinogenic agents. The clinical relevance of the latter observation is not known.
Fertility studies in rodents and primates have shown that treatment with Nebido 1000mg/4 ml can impair fertility by suppressing spermatogenesis in a dose-dependent manner.
How should I take Nebido 1000mg/4 ml?
Your doctor will test the Nebido 1000mg/4 ml levels in your blood before you start and while you are using Nebido 1000mg/4 ml.
Nebido 1000mg/4 ml comes with a patient information leaflet. Read and follow these instructions carefully. Ask your doctor if you have any questions.
Nebido 1000mg/4 ml is for use only in the nose. Do not get any of it in your eyes or on your skin. If it does get on these areas, rinse it off right away.
To use:
If you are using Nebido 1000mg/4 ml for the first time, you will need to prime the pump. To do this, hold the Natesto® pump over a sink, turn it upside down, and slowly press the pump for 10 times.
If any medication comes out during priming, discard it into the sink and rinse down the drain with warm water.
Wipe the tip with a clean, dry tissue if there is any medicine left on the tip of the pump. Now it is ready to use.
If you get the medicine on your hands, wash it away with warm water and soap.
Gently blow your nose to clear the nostrils.
While looking in the mirror, insert the tip of the pump into your left nostril and gently tilt it so that it touches the side wall of your nostrils to ensure it is applied properly.
Slowly press the pump until it stops and remove the tip slowly from your nose.
Do the same steps applying the medicine into your right nostril.
After using the pump, wipe the tip with a clean, dry tissue and put the cap back on.
Press your nostrils together just below the middle of your nose and lightly rub them together.
Do not blow your nose or sniff 1 hour after using Nebido 1000mg/4 ml.
Dosing
The dose of Nebido 1000mg/4 ml will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Nebido 1000mg/4 ml. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
For nasal dosage form (gel):
For hormone replacement:
Adults—11 milligrams (mg), or 1 pump actuation in each nostril, three times a day (once in the morning, once in the afternoon, and once in the evening, about 6 to 8 hours apart).
Children—Use and dose must be determined by your doctor.
Missed Dose
If you miss a dose of Nebido 1000mg/4 ml, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Storage
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Nebido 1000mg/4 ml administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
sponsored
Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.
Apply the Nebido 1000mg/4 ml topical (transdermal) patch to a flat, clean, dry, and undamaged area of skin on your back, stomach, upper arm, or thigh. Wear the patch for 24 hours and then replace it with a new patch. Apply your patch at the same time each evening.
Choose a different skin area to wear each new patch you put on. You should not use the same skin area twice in a 7-day period.
After removing a patch, fold it closed with the sticky side in, and throw it away in a place where pets and children cannot reach it.
Apply the Nebido 1000mg/4 ml gel at the same time each day (preferably in the morning) to clean, dry, unbroken skin on the shoulders or upper arms. Open the gel pouch, and squeeze the entire contents onto the palm of your hand. Apply the gel right away and allow it to dry for at least 5 minutes before you dress. Wash your hands with soap and water after applying the gel.
Do not apply Nebido 1000mg/4 ml gel to your penis or your scrotum. The Nebido 1000mg/4 ml brand of Nebido 1000mg/4 ml gel should also not be applied to your stomach area.
It is best to cover treated skin areas with clothing while using Nebido 1000mg/4 ml gel. This will help prevent getting this medicine on other people. If someone else does come into contact with a treated skin area, they must wash the contact area right away with soap and water.
To be sure this medicine is helping your condition, your blood will need to be tested often. Your prostate or liver function may also need to be tested. Visit your doctor regularly.
Use Nebido 1000mg/4 ml topical regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.
Store at room temperature away from moisture and heat. Keep each skin patch in the foil pouch until you are ready to use it. Do not use a skin patch that has been cut or damaged.
Nebido 1000mg/4 ml pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
sponsored
Mechanism of Action
Endogenous androgens, including Nebido 1000mg/4 ml and dihydrotestosterone (DHT), are responsible for the normal growth and development of the male sex organs and for maintenance of secondary sex characteristics. These effects include the growth and maturation of prostate, seminal vesicles, penis and scrotum; the development of male hair distribution, such as facial, pubic, chest and axillary hair; laryngeal enlargement, vocal chord thickening, alterations in body musculature and fat distribution. Nebido 1000mg/4 ml and DHT are necessary for the normal development of secondary sex characteristics.
Male hypogonadism, a clinical syndrome resulting from insufficient secretion of Nebido 1000mg/4 ml, has two main etiologies. Primary hypogonadism is caused by defects of the gonads, such as Klinefelter’s Syndrome or Leydig cell aplasia, whereas secondary hypogonadism is the failure of the hypothalamus (or pituitary) to produce sufficient gonadotropins (FSH, LH).
Pharmacodynamics
No specific pharmacodynamic studies were conducted using Nebido 1000mg/4 ml Gel 1%.
Pharmacokinetics
Absorption
Nebido 1000mg/4 ml Gel 1% delivers physiologic amounts of Nebido 1000mg/4 ml, producing circulating Nebido 1000mg/4 ml concentrations that approximate normal concentrations (298 to 1043 ng/dL) seen in healthy men. Nebido 1000mg/4 ml Gel 1% provides continuous transdermal delivery of Nebido 1000mg/4 ml for 24 hours following a single application to intact, clean, dry skin of the shoulders, upper arms and/or abdomen.
Nebido 1000mg/4 ml Gel 1% is a hydroalcoholic formulation that dries quickly when applied to the skin surface. The skin serves as a reservoir for the sustained release of Nebido 1000mg/4 ml into the systemic circulation. Approximately 10% of the Nebido 1000mg/4 ml dose applied on the skin surface from Nebido 1000mg/4 ml Gel is absorbed into systemic circulation. In a study with Nebido 1000mg/4 ml Gel 1% 100 mg, all patients showed an increase in serum Nebido 1000mg/4 ml within 30 minutes, and eight of nine patients had a serum Nebido 1000mg/4 ml concentration within normal range by 4 hours after the initial application. Absorption of Nebido 1000mg/4 ml into the blood continues for the entire 24-hour dosing interval. Serum concentrations approximate the steady-state concentration by the end of the first 24 hours and are at steady state by the second or third day of dosing.
With single daily applications of Nebido 1000mg/4 ml Gel 1%, follow-up measurements 30, 90 and 180 days after starting treatment have confirmed that serum Nebido 1000mg/4 ml concentrations are generally maintained within the eugonadal range. Figure 1 summarizes the 24-hour pharmacokinetic profiles of Nebido 1000mg/4 ml for hypogonadal men (less than 300 ng/dL) maintained on Nebido 1000mg/4 ml Gel 1% 50 mg or 100 mg for 30 days. The average (± SD) daily Nebido 1000mg/4 ml concentration produced by Nebido 1000mg/4 ml Gel 1% 100 mg on Day 30 was 792 (± 294) ng/dL and by Nebido 1000mg/4 ml Gel 1% 50 mg 566 (± 262) ng/dL.
Figure 1: Mean (± SD) Steady-State Serum Nebido 1000mg/4 ml Concentrations on Day 30 in Patients Applying Nebido 1000mg/4 ml Gel 1% Once Daily
Distribution
Circulating Nebido 1000mg/4 ml is primarily bound in the serum to sex hormone-binding globulin (SHBG) and albumin. Approximately 40% of Nebido 1000mg/4 ml in plasma is bound to SHBG, 2% remains unbound (free) and the rest is bound to albumin and other proteins.
Metabolism
Nebido 1000mg/4 ml is metabolized to various 17-keto steroids through two different pathways. The major active metabolites of Nebido 1000mg/4 ml are estradiol and dihydrotestosterone (DHT).
DHT concentrations increased in parallel with Nebido 1000mg/4 ml concentrations during Nebido 1000mg/4 ml Gel 1% treatment. The mean steady-state DHT/T ratio during 180 days of Nebido 1000mg/4 ml Gel treatment ranged from 0.23 to 0.29 (50 mg of Nebido 1000mg/4 ml Gel 1%/day) and from 0.27 to 0.33 (100 mg of Nebido 1000mg/4 ml Gel 1%/day).
Excretion
There is considerable variation in the half-life of Nebido 1000mg/4 ml concentration as reported in the literature, ranging from 10 to 100 minutes. About 90% of a dose of Nebido 1000mg/4 ml given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of Nebido 1000mg/4 ml and its metabolites. About 6% of a dose is excreted in the feces, mostly in the unconjugated form. Inactivation of Nebido 1000mg/4 ml occurs primarily in the liver.
When Nebido 1000mg/4 ml Gel 1% treatment is discontinued after achieving steady state, serum Nebido 1000mg/4 ml concentrations remain in the normal range for 24 to 48 hours but return to their pretreatment concentrations by the fifth day after the last application.
Nebido 1000mg/4 ml Transfer from Male Patients to Female Partners
The potential for dermal Nebido 1000mg/4 ml transfer following Nebido 1000mg/4 ml Gel 1% use was evaluated in a clinical study between males dosed with Nebido 1000mg/4 ml Gel 1% and their untreated female partners. Two (2) to 12 hours after application of 100 mg of Nebido 1000mg/4 ml administered as Nebido 1000mg/4 ml Gel 1% by the male subjects, the couples (N = 38 couples) engaged in daily, 15-minute sessions of vigorous skin-to-skin contact so that the female partners gained maximum exposure to the Nebido 1000mg/4 ml Gel 1% application sites. Under these study conditions, all unprotected female partners had a serum Nebido 1000mg/4 ml concentration >2 times the baseline value at some time during the study. When a shirt covered the application site(s), the transfer of Nebido 1000mg/4 ml from the males to the female partners was completely prevented.
References
DailyMed. "TESTOSTERONE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
NCIt. "Therapeutic Testosterone: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
EPA DSStox. "Testosterone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
The results of a survey conducted on ndrugs.com for Nebido 1000mg/4 ml are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Nebido 1000mg/4 ml. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.
User reports
Consumer reported administration
No survey data has been collected yet
Consumer reviews
There are no reviews yet. Be the first to write one!
