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Pentobarbital Addiction, Effects, and Treatment

PENTOBARBITAL ADDICTION, EFFECTS, AND TREATMENT 11

PentobarbitalAddiction, Effects, and Treatment

PentobarbitalAddiction, Effects, and Withdrawal

Theuse of Pentobarbital in medical settings to treat psychologicaldisorders such as hyperactivity of brain, insomnia and even sometimesto sedate patients before surgery procedures pose challenges to theAmericans. The reason for this is that like other drugs of abuse,Pentobarbital is used in other ways not medically necessary toachieve euphoria (feeling high) and enjoyment. Also, the dependencyon this drug can be worse than that of hard drugs such as crystalmeth and cocaine. Patients undergoing medication involvingprescription of pentobarbital becomes addicts in the ways not easy tosuspect because its mental effects are usually mistaken with the sideeffects of the treatment or the symptoms of the surgery procedure orbrain hyperactivity (Ziemba &amp Forman, 2016). For this reason,most people realize when they have already developed a dependency onthe drug. In such conditions, medical attention is necessary to treatthe addiction before it persists to the need of high doses forsatisfaction.The potential dangers pentobarbital poses to the American youthsnecessitates strengthening of drug policies and proper management ofboth patients and the drugs sold in pharmacies to prevent not onlyaddiction but also its social, economic and mental impacts to theAmerican societies.

TheProperties and Uses of Pentobarbital

Pentobarbitalbelongs to the class of barbiturates (Ajemni etal.,2015). These are drugs used to treat increased anxiety, insomnia, anddepression. Due to the expansion of knowledge in psychopharmacologyfield, this drug has been reported to be useful in emergencytreatment for seizures and surgical practices as antidepressant. Thereason behind Pentobarbital addiction is that it slows down the brainactivity and central nervous system to give a sense of peace,satisfaction, hypnosis, and enjoyment (Ainsworth, 2011). Consequently, the patient undergoing the treatment may continue touse them even after the original medical condition is healed.Although pentobarbital is intended for short term use, theiraddiction can be permanent if medical care is not provided, leadingto reduced reasoning, sensitivity to hunger and coordination.

Thechemical composition of pentobarbital (C11H18N2O3)comprises of carbon, hydrogen, and oxygen as key elements-(pentobarbital | C11H18N2O3– PubChem, 2016). The compound is mostly available in forms ofPentobarbital sodium salts (with empirical formula C11H17N2NaO3)and is regarded as a strong neurochemical (pentobarbital | C11H18N2O3– PubChem, 2016). This is the basis for which the drug is used inclinical settings and illegally as narcotics. Consequently, the USDrug Enforcement Agency (DEA) has classified it as a Schedule IIsubstance (Ainsworth, 2011). All the controlled substances includingthe morphine, methadone, and codeine belong to this category.

TheHistory of Pentobarbital

Thehistory of barbiturates began long before their clinical introductionin the year 1904, the year Farbwerke Bayer and Company came up withthe first chemical that was used in many pharmacological, psychiatricand neurological disorders (Ainsworth, 2011). Many patients couldreceive treatment and therapies especially those with neuroses,emotional repression, and psychoses. Later, numerous other suchchemicals were discovered, and their effectiveness in sedative,hypnotic and anticonvulsant goals acknowledged. By the 20th century,more than 2500 barbiturates were already known, studies and theircontributions documented (Ainsworth, 2011). However, only 50chemicals were used in clinical practices.

Theglobal attention to the importance of pentobarbital came with thediscovery of its use in lethal injection in America during the lasthalf of the nineteenth century. Numerous studies documented that thedrug can be used in euthanasia and execution when used alone in highdoses or as a complementary chemical with phenytoin. As a euthanasiaagent, 10 g are administered in liquid form to the patients followedby a bromine solution to execute induced respiratory arrest(Ainsworth, 2011). Consequently, the victim or individual couldsuccumb to a slow and painless death. Specifically, Texas has beenusing pentobarbital to execute capital punishment victims since 2012(Trubuhovich, 2015). Other states using the chemical includesCalifornia, Washington, Ohio and Arizona. In the last one decade,the medical and scientists have also discovered many other uses ofpentobarbital chemical, leading to the discovery of abuse andeffects.

Movementand Distribution of Pentobarbital (Pharmacokinetics)

Physically,the drug is in forms of crystalline granules or a fine white powder(Ajemni etal.,2015). It can dissolve in water or other solvents in preparation foruse as through injection. In most clinical cases, pentobarbital isadministered orally or intravenous as injections. Once the chemicalis in the body, the distribution can occur through a centralcompartment or peripheral compartment (Ziemba &amp Forman, 2016).These two compartments have different impacts on the patients. Also,their concentration in the body also differs. For example, theperipheral compartment was found to increase the body weight of theusers. In a study by Jelliffe etal.(2015), the total amount of pentobarbital in the central compartmentwas about 87 percent while the systemic circulation held about 13percent. Water plasma and plasma protein in the blood distributed wasabout 4 percent and 5 percent respectively.

MostBarbiturates are metabolized by the enzymes in the microsomal systemand the byproducts removed through urine and fecal matter. Theseexcretion processes remove about 25-50 percent of the originalPentobarbital dosage (Hosseini etal.,2014). The rest is absorbed and distributed throughout the bodythrough the central or peripheral compartments, leading to behavioralmodification and physical symptoms (Trubuhovich, 2015). Pentobarbitalexists in circulation as weak acids that are easily and quicklydistributed to body tissues and fluids. Most of the concentrationusually settles in the brain, liver, and kidneys (Jelliffe etal.,2015). While the rate of distribution and penetration to tissuesdepends on the solubility, their effectiveness as the drug of addictrelies on their influence on the central nervous system.

Asa barbiturate, pentobarbital acts in a selective mode on thegamma-amino butyric acid-A (GABA-A) brain receptors, therebyinhibiting or reducing the activities of the neurons. GABA chemicalmessengers are plenty in the blood cells and have the capability tobind on the neurons and consequently reduce their activities. Psychologically, (GABA-A) receptors are associated with the feelingsof fear, anxiety, and anger (pentobarbital | C11H18N2O3– PubChem, 2016 Pentobarbital – DrugBank, 2016). They are commonin human nervous system and facilitate more than 40 percent ofsynapses in the brain. Also, they influence person’s cognitionability by facilitating the glutamatergic processes. Once thePentobarbital is in the brain, it opens the GABA- activated channelsand allows the chloride ions to penetrate the neurons in the CNS(Ziemba &amp Forman, 2016). These ions make the neurons to becomenegatively charged thereby rendering them resistance to excitation.As a result, the entire network of GABA receptors becomesunresponsive to the signals of anger and anxiety (Ziemba &ampForman, 2016). Such effect is like shutting off one’s sensitivesystems, the idea behind the clinical use during surgery and asantidepressants. GABA-A receptors and GABA messengers achieve theinhibition process through a “lock” and “key” mechanism. Forthis reason, they are said to be selective of functional specific.

However,this chemical has a short half-life, and it decomposes after about20-24 hours. For this reason, the patient or addict will have totake another dose to retain the euphoria or avoid insomnia andanxiety (Trubuhovich, 2015). When mixed with other substances such asalcohol, the manifestation may take longer to disappear (Hosseini etal.2014). Over the course of time, the user becomes aware of rapidlydisappearing euphoria as the body becomes highly dependent onpentobarbital, this prompt most people to increase the dosage toextend the relaxation and satisfaction. This is the major reason forpentobarbital overdose, leading to the mortality of significantyouths annually.

TheEffects of Pentobarbital (Pharmacodynamics)

Asmentioned earlier in this study, Pentobarbital is clinically used totreat short-term insomnia among other psychological issues. In ageneral case, it targets on the central nervous system and depressesthe neurons to induce drowsiness and relieve the nervousness. Also,using Pentobarbital can result in excitation.

Pentobarbitaloperates on binding sites where GABAA receptors and chlorine ions arelocated. Also, it slows the transmission thereby increasing theperiod which these ions are active for neurons inhibition(pentobarbital | C11H18N2O3 – PubChem, 2016). The chlorine ionsare negatively charged, and when they enter neurons, they reducetheir sensitivity to excitation. Consequently, the inhibition actionof the GABAA receptors and the GABA chemicals inside the thalamus areprolonged. The two factors act in &quotlock&quot and &quotkey&quotmechanism to induce the neuron resistance (Pentobarbital –DrugBank, 2016). Pentobarbital and other barbiturates usuallyfunction through a potent and direct inhibition process of theα-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPAR)receptors. These receptors actively mediate the transmission ofsynapses within the CNS (Pentobarbital – DrugBank, 2016). Theinhibition results in the suppression of the neurons and theirglutamatergic transmission, leading to nerves resistance for a perioddictated by the half-life of the insoluble Pentobarbital incirculation. In the case of overdose, the suppression can continuefor a long time leading to the surfacing of sluggishness,incoordination, and retarded speech.

Thefactors that determine the effects of pentobarbital in humans are thesolubility of the substance in the blood system and also theconcentration gradient between the blood and the tissues (Chan &ampAnderson, 2014). Also, the perfusion through the tissues alsoinfluences variants of the Pentobarbital chemicals in the body. Forinstance, the soluble pentobarbital can be already in the blood andbrain system, but there is the short time before the anestheticeffect. This short term is determined by the way these chemicals aredelivered in the capillary bed of the brain tissues. For this reason,Chan and Anderson (2014) explains that the time to the onset of thedrug effect is due to the chemical characteristics of the drug andthe significant level of the cardiac injection into the brain. Oncethe drug molecules have been delivered into the brain tissues,effects occur in Central Nervous System, Cardiovascular, andPulmonary Systems.

Whenused as a prescription drug or for addiction purposes, Pentobarbitalexhibits a wide range of symptoms. To the brain, it depresses thecerebral metabolism leading to a lack or loss of memory,concentration, balance, and coordination between brain and body partssuch as hands (Ainsworth, 2011). Also, the speech deteriorates whileboth heart rate and breathing become weak and shallow. Due to theexperience of euphoria, the user may start hallucinating and finallypass out.

Thecardiovascular system is also affected by the presence ofPentobarbital in the blood system. Consequently, peripheralvasodilation occurs due to the decreased preload caused by thereduced cardiac output. This symptom is serious in the patients whohave a hypertensive response, ischemic stroke and myocardial diseases(Ainsworth, 2011). In this case, persistence use can lead toincreased severity of these diseases and finally death due to suddenevents such as ischemic stroke and sudden heart attack. Also, theusers may excrete reduced urine that is influenced by reduced bloodflow and shivering due to increased heat loss that is an impact ofvasodilation. Other fewer effects of using Pentobarbital include thenightmares, nausea, constipation unnecessary excitement, andaggression. Moreover, one may have a headache, feeling of hangover ordrowsiness one day after a dose.

TheTreatment and Withdrawal of Pentobarbital

Pentobarbitalwithdrawal involves administration of medicine that will work on thenervous system first in a way similar to the pentobarbital drug. Suchtreatment is referred to as detoxification (Trubuhovich, 2015)However, most of the medicine used does not have addictivecharacteristics such as those of pentobarbital. Also, they do notremove the toxins of pentobarbital but instead reduces the dependencyon the drug.

Thewithdrawal treatment of pentobarbital is an inpatient activity. Inthis case, self-patient management is the key to the recovery.However, in cases of emergency, the patient can be taken to ahospital facility where there is sufficient medical attention(Trubuhovich, 2015). Most rehabilitation doctors and officerspreferred subjecting the patient in detox processes at theresidential treatment facility. The reason for this is that a localor home environmental setting contributes to the recovery of thepatients particularly in the initial stages of the treatment.

Themost challenging recovery process is the treatment of addiction.Unlike withdrawal treatment, addiction requires receiving health careon the outpatient basis (Trubuhovich, 2015). In this case, thepatient should register with a rehabilitation institution where theycan receive complete treatment course which included medication andbehavioral adjustments. However, in the cases the patient seemsmotivated towards recovery or the addiction is a mild condition, onecan be allowed to take an inpatient treatment course.

Inbrief, pentobarbital is a dangerous drug unless when administeredunder highly controlled circumstances that will enable detection ofany sign of dependency or inappropriate use. Many patients undergoingpsychological therapies have discovered their addiction when it isalready too late. However, early medical interventions are highsuccessful and can help a patient withdraw from the dependency beforeit progresses. Also, institutional and governmental control ofpentobarbital and other barbiturates can help reduce addiction andthe mortality rate among the youths. Also, diseases such as coronaryartery disease and stroke that deteriorate with increased addictioncan be prevented and managed. Finally, ample research is necessary todevelop ways in which the dependency effect of barbiturates use inclinical settings can be stemmed out to ensure that patients are notdeveloping the addiction in the course of their treatment.

References

Ainsworth,S. (2011). Barbiturates: soldiers, saints and spies. PracticeNurse,41(6), 32-33.

Ajemni,M., Balde, I., Kabiche, S., Carret, S., Fontan, J., Cisternino, S., &ampSchlatter, J. (2015). Stability-Indicating Assay for theDetermination of Pentobarbital Sodium in Liquid Formulations.InternationalJournal of Analytical Chemistry,20151-6. doi:10.1155/2015/697937

Chan,L., &amp Anderson, G. (2014). Pharmacokinetic and PharmacodynamicsDrug Interactions with Ethanol (Alcohol). ClinicalPharmacokinetics,53(12), 1115-1136. Doi: 10.1007/s40262-014-0190-x

Hosseini,A., Ghorbani, A., Sadeghnia, H. R., Rajabian, A., &amp Rakhshandeh,H. (2014). Potentiating effects of Lactuca serriola onpentobarbital-induced sleep. ResearchOpinions in Animal &amp Veterinary Sciences,4(11), 601-607

Jelliffe,R., Milman, M., Schumitzky, A., Bayard, D., &amp Van Guilder, M.(2015). “ATwo-Compartment Population Pharmacokinetic–Pharmacodynamics Modelof Digoxin in Adults, With Implications for Dosage.” NationalInstitute of Health

Pentobarbital- DrugBank.(2016). Drugbank.ca.Retrieved 26 November 2016, fromhttps://www.drugbank.ca/drugs/DB00312#taxonomy

Pentobarbital| C11H18N2O3 – PubChem. (2016). Pubchem.ncbi.nlm.nih.gov. Fromhttps://pubchem.ncbi.nlm.nih.gov/compound/pentobarbital#section=Top

Trubuhovich,R. V. (2015). Pioneering early Intensive Care Medicine by the`Scandinavian Method` of treatment for severe acute barbituratepoisoning. Anaesthesia&amp Intensive Care,4329-39

Ziemba,A. M., &amp Forman, S. A. (2016). Correction for Inhibition Leads toan Allosteric Co-Agonist Model for Pentobarbital Modulation andActivation of α1β3γ2L GABAA Receptors. PlosONE,11(4), 1-14. doi:10.1371/journal.pone.0154031