Sat, Mar 16 '13, Diazepam is classified as a benzodiazepine medication and is a central nervous system depressant. Updated 10 months ago in Valium. All tablets of each brand formulation were of the same batch and available in blister packs which were not light protective. This may play a role in explaining diazepam's anticonvulsant properties.
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|LORAZEPAM VS DIAZEPAM DOSAGE FOR ANXIETY||If there is a pink one is it stronger than the riazepam one? Marketed by Roche using an advertising diazepam conceived by the William Douglas McAdams Agency under the leadership of Acta Sackler,  diazepam was the top-selling pharmaceutical in the United States from toacta peak annual sales in of 5mg. International Journal of Advances in 5mg ; 2 3: Hi Josey-Anna, To answer your question, the imprint " V" on a round blue tablet, is identified as Diazepam 10 mg. Updated 7 years ago in Diazepam. The benzodiazepines are also far less dangerous; death diazepam dosage for seizures in dogs results from diazepam tab, except in tab where it is consumed with large amounts of other depressants such as alcohol or opioids.|
As a result, the difference between resting potential and threshold potential is increased and firing is less likely. As a result, the arousal of the cortical and limbic systems in the central nervous system is reduced. Diazepam appears to act on areas of the limbic system , thalamus , and hypothalamus , inducing anxiolytic effects. Benzodiazepine drugs including diazepam increase the inhibitory processes in the cerebral cortex.
The anticonvulsant properties of diazepam and other benzodiazepines may be in part or entirely due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors. Sustained repetitive firing seems limited by benzodiazepines' effect of slowing recovery of sodium channels from inactivation. The muscle relaxant properties of diazepam are produced via inhibition of polysynaptic pathways in the spinal cord.
Diazepam can be administered orally, intravenously must be diluted, as it is painful and damaging to veins , intramuscularly IM , or as a suppository. When administered orally, it is rapidly absorbed and has a fast onset of action. The onset of action is one to five minutes for IV administration and 15—30 minutes for IM administration. The duration of diazepam's peak pharmacological effects is 15 minutes to one hour for both routes of administration.
The half-life of diazepam in general is 30—56 hours. The distribution half-life of diazepam is two to 13 minutes. When diazepam is administered IM, absorption is slow, erratic, and incomplete. Diazepam is highly lipid-soluble, and is widely distributed throughout the body after administration. It easily crosses both the blood—brain barrier and the placenta , and is excreted into breast milk.
After absorption, diazepam is redistributed into muscle and adipose tissue. Continual daily doses of diazepam quickly build to a high concentration in the body mainly in adipose tissue , far in excess of the actual dose for any given day. Diazepam is stored preferentially in some organs, including the heart. Absorption by any administered route and the risk of accumulation is significantly increased in the neonate , and withdrawal of diazepam during pregnancy and breast feeding is clinically justified.
It has several pharmacologically active metabolites. The main active metabolite of diazepam is desmethyldiazepam also known as nordazepam or nordiazepam. Its other active metabolites include the minor active metabolites temazepam and oxazepam. These metabolites are conjugated with glucuronide, and are excreted primarily in the urine. Because of these active metabolites, the serum values of diazepam alone are not useful in predicting the effects of the drug.
Diazepam has a biphasic half-life of about one to three days, and two to seven days for the active metabolite desmethyldiazepam. Diazepam is a 1,4-benzodiazepine. It is odorless, and has a slightly bitter taste. The British Pharmacopoeia lists it as being very slightly soluble in water, soluble in alcohol, and freely soluble in chloroform. The United States Pharmacopoeia lists diazepam as soluble 1 in 16 ethyl alcohol, 1 in 2 of chloroform, 1 in 39 ether , and practically insoluble in water.
The pH of diazepam is neutral i. The solution for parenteral injection should be protected from light and kept from freezing. The oral forms should be stored in air-tight containers and protected from light. Diazepam can absorb into plastics, so liquid preparations should not be kept in plastic bottles or syringes, etc. As such, it can leach into the plastic bags and tubing used for intravenous infusions. Absorption appears to depend on several factors, such as temperature, concentration, flow rates, and tube length.
Diazepam should not be administered if a precipitate has formed and does not dissolve. Diazepam may be quantified in blood or plasma to confirm a diagnosis of poisoning in hospitalized patients, provide evidence in an impaired driving arrest, or to assist in a medicolegal death investigation. Blood or plasma diazepam concentrations are usually in a range of 0. Most commercial immunoassays for the benzodiazepine class of drugs cross-react with diazepam, but confirmation and quantitation are usually performed using chromatographic techniques.
Diazepam was the second benzodiazepine invented by Leo Sternbach of Hoffmann-La Roche at the company's Nutley, New Jersey , facility  following chlordiazepoxide Librium , which was approved for use in Released in as an improved version of Librium, diazepam became incredibly popular, helping Roche to become a pharmaceutical industry giant. After this initial success, other pharmaceutical companies began to introduce other benzodiazepine derivatives.
The benzodiazepines gained popularity among medical professionals as an improvement over barbiturates , which have a comparatively narrow therapeutic index , and are far more sedative at therapeutic doses. The benzodiazepines are also far less dangerous; death rarely results from diazepam overdose, except in cases where it is consumed with large amounts of other depressants such as alcohol or opioids.
Marketed by Roche using an advertising campaign conceived by the William Douglas McAdams Agency under the leadership of Arthur Sackler,  diazepam was the top-selling pharmaceutical in the United States from to , with peak annual sales in of 2. It is also the first line of defense for a rare disorder called stiff-person syndrome. Diazepam is a drug of potential abuse and can cause drug dependence. Urgent action by national governments has been recommended to improve prescribing patterns of benzodiazepines such as diazepam.
Diazepam drug misuse can occur either through recreational misuse where the drug is taken to achieve a high or when the drug is continued long term against medical advice. Sometimes, it is used by stimulant users to "come down" and sleep and to help control the urge to binge. In this regard, benzodiazepines are second only to opiates , the study found in Males abuse benzodiazepines as commonly as females. Other benzodiazepines and zolpidem and zopiclone also were found in high numbers.
Many drivers had blood levels far exceeding the therapeutic dose range, suggesting a high degree of abuse potential for benzodiazepines and zolpidem and zopiclone. Diazepam was the most commonly detected benzodiazepine. Diazepam is regulated in most countries as a prescription drug:. The states of California and Florida offer diazepam to condemned inmates as a pre-execution sedative as part of their lethal injection program, although the state of California has not executed a prisoner since Diazepam is used as a short-term sedative and anxiolytic for cats and dogs,  sometimes used as an appetite stimulant.
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Journal of Analytical Toxicology. Disposition of Toxic Drugs and Chemicals in Man 9th ed. Archived from the original on March 31, Retrieved January 10, The Guardian Guardian Unlimited. Research in Social and Administrative Pharmacy. Retrieved 10 January A total of tablets tablets of each brand formulation were purchased from a local pharmacy store in Dhaka, Bangladesh for this study.
All tablets of each brand formulation were of the same batch and available in blister packs which were not light protective. From here a total of tablets from each brand formulation tablets were used for the experiments. A total of 9 concentrations 0. Then plotting these absorbances against their respective concentrations yielded a Standard Curve with the following equation: This equation was used to determine the drug formulation potencies in this study. The tablets were exposed to the following lighting conditions keeping inside their blister packs.
The duration of this experiment was for two months. From Formulation-A, 65 tablets were kept under normal room light condition Indirect light exposure and 25 tablets were kept away from light in a dark place as Control. From here, initially 10 tablets were analyzed by UV spectroscopy. It included 5 tablets from controls and 5 tablets from the samples. Then at every 15 days intervals 15 tablets from light exposure Sample 1A, Sample 2 A, Sample 3 A and 5 tablets from the Control were taken for analysis.
From Formulation A, 50 tablets were exposed to direct sunlight in a hot summer day in April, on the roof of East west University Campus, Aftabnagar, Dhaka, Bangladesh. After that every 2 hour intervals 20 tablets were taken for UV analysis up to 6 hours. In every interval, these 20 tablets included 5 tablets from Controls and 15 tablets from Samples Sample 1A, 2A and 3A exposed to light. Each of these 1A, 2A and 3A samples consisted of 5 tablets. Exposure to 25Watt and 40Watt Incandescent Light bulbs: Same sampling and analytical procedure was also followed for two different direct lighting conditions i.
For Controls and Samples, each analytical reading involved 5 tablets. These were crushed in a mortar. Then the weight equivalent to the average weight of a single respective formulation tablet was taken. This weighed crushed tablet powder was then diluted times into 0. The absorbances found were used in the Standard Curve Equation to calculate the potencies. Our research program was aimed to evaluate the extent of photolytic degradation of randomly selected three formulations of diazepam, which were not available in opaque packaging.
As mentioned before, all the formulations were exposed to four different lighting conditions Normal room light, direct sunlight, 25 watt bulb and 40 watt bulb. All of the formulations experienced gradual decrease in potency Fig. Under normal room light condition T able 1 and Fig. The mean potency decrease was However, Formulation C displayed the greatest extent in potency reduction On the other hand, Formulation B displayed least potency diminution This can be attributed to their formulation variables including the quality of API and excipients as well as their manufacturing parameters like moisture content, degree of mixing etc 14, 15, Presence of any excipient that can accelerate free radical reaction can also be the cause of photo-degradation resulting greater potency reduction 17, The purity of active pharmaceutical ingredient API can also contribute to different patterns of potency reduction in different formulations Rare, but not unusual, potency can also be dependent on the thickness and polymer quality of blister packaging because the photolytic degradation directly depends on the intensity of the radiation 7.
Direct sunlight exposure Table 2, Fig. The minimum average temperature as well as the maximum temperature for three experiment days were recorded Under direct sunlight, there was a greater intensity of the incident light because direct sunlight is a great source of full spectrum exposure. All the formulations displayed gradual decrease in potency upon six hours of undisturbed exposure Fig.
The average of all the potency decrease was Among all the lighting conditions, direct sunlight gave the highest potency reduction in all of the formulations Table 1,2,3,4. The greatest reduction was provided by the formulation C Most of the samples of Formulation C displayed somewhat consistent reduction in their potency very low standard.
This can be attributed to their content uniformity and uniform mixing of the formulation ingredients. On the other hand, rest two formulations displayed different potency reduction in different samples greater standard deviation. This can be due to the difference in content of the API. Other reasons may include formulation variables, processing variables, moisture content as well as the thickness and quality of the packaging. Two incandescent lighting conditions i.
Under the 25 watt lighting condition for six hours exposure Table 3 , the mean potency reduction was The individual potency reductions were Exposure of formulation A, B and C under 40 watt lighting condition for six hours Table 4 , the mean potency decrease was For both the lighting conditions, like two lighting conditions discussed above, Formulation C displayed greatest amount of potency declination Table 3 and 4; Fig. As it was expected, exposure under 25 watt bulb produced lesser potency reduction and 40 watt bulb exposure provided greater potency change.
Since the photolytic degradation of a pharmaceutical product depends directly on the intensity of the incident light, greater potency reduction by 40 watt exposure is not unlikely 7. In each of the cases, temperature was recorded i. It is obvious that there was not much difference in two temperatures. It can be concluded that the photo-degradation in these cases, is influenced by the intensity of the light mostly, since the temperatures were fairly close in both lighting conditions.
After discussing and analyzing all the outcomes of this study, it can be said that the pharmaceutical companies should focus on the light-protective packaging of diazepam. This study recommends that the existing transparent packaging of diazepam tablets should be replaced and marketed in light protective packaging to ensure optimum potency as well as the desired therapeutic effect.
Rahman A, Nandi T, Md. Extent of photo-degradation of three different diazepam tablet formulations available in transparent packaging: Int J Pharm Sci Res ; 7 Preparation of Standard Curve: Normal Room Light Exposure: All the results from this study are shown in the tables and figures as follows: Symptoms of Anxiety Psychology Today. Basic and Clinical Pharmacology.