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Dexmedetomidine

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Recommended: Pharmacological properties of dexmedetomidine

PHARMACOLOGY OF DEXMEDETOMIDINE Dexmedetomidine HCl, an imidazole compound is the pharmacologically active s-enantiomer of medetomidine, a veterinary anaesthetic agent. It is described chemically as (+)-4-(s)[2 3 –(dimethylphenyl) ethyl]-11 H-imidazole monohyrochloride. Its empirical formula is C13H16N2HCl and its molecular weight is 236.7(57). Figure 4 : Structure of Dexmedetomidine PHYSIOCHEMICAL PROPERTIES A white or almost white powder that is freely soluble in water with Pka of 7.1.Partition coefficient in octanol: water at pH 7.4 is 2.89. Preservative free dexmedetomidine is available in 1ml and 2 ml ampoule as Dexmedetomidine Hydrochloride for intravenous use (Alphadex, Fusion health care 100 μg/ml). It can also be used for intrathecal and epidural anaesthesia. MECHANISM OF ACTION OF DEXMEDETOMIDINE Dexmedetomidine is the dextro enantiomer of medetomidine, the methylated derivative of etomidine, its specificity for the alpha-2 receptor is 8times that of clonidine, with an alpha-2/alpha-1 binding affinity ratio of 1620:1 & its effects are dose dependently reversed by …show more content…

Alpha-2 adrenoceptors are found in CNS in highest densities in the locus ceruleus, the predominant noradrenergic nuclei of the brainstem and an important modulator of vigilance. Presynaptic activation of alpha-2A adrenoceptor in the locus ceruleus inhibits the release of nor-epinephrine & results in the sedative and hypnotic effects(62). In addition, the locus ceruleus is the site of origin for the descending medullospinal nor adrenergic pathway, known to be an important modulator of nociceptive neurotransmission. Stimulation of alpha-2 adrenoceptors in this area terminates the propagation of pain signals leading to analgesia. Postsynaptic activation of alpha-2 receptors in the CNS results in decrease in sympathetic activity leading to hypotension &

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Limaye PMCY 6510 Take Home Final Exam Metformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is a white to off-white crystalline compound with a molecular formula of C4H11N5•HCl and a molecular weight of 165.63. Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. Metformin belongs to BCS class III with high solubility and low permeability. This also allows for designing a controlled release formulation of metformin hydrochloride. However, due to the high dose amounts and dosing frequency, it has been a challenge to develop once daily metformin formulation.

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Dosage 10-30mg q24h/ 5-20mg q4-6h/ IV 2.5-15mg. Drug indication/uses To treat moderate to severe pain, cough suppression, to treat diarrhea, anesthesia, acute pulmonary edema, cancer pain. Drug action Binds to Mu receptor and inhibits substance P in CNS. Contraindication Severe asthma, increases intracranial pressure, pregnancy, respiratory depression.

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Question / Problem: What is the evidence to recommend Trulicity (dulaglutide) to a patient who has uncontrolled glucose control, and is on metformin and insulin (levemir) and non- adherence to the insulin. Response: The trulicity is a non-insulin injectable with dosing regimen of once weekly dosing. These agents work by activating GLP-1 receptors in the pancreas, which leads to enhanced insulin release and reduced glucagon release-responses that are both glucose-dependent-with a consequent low risk for hypoglycemia.

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It is an antagonist that irreversibly blocks the vesicular monoamine transporters (VMAT) on neurons in the CNS. It blocks the transport of Noradrenaline into the synaptic

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Since opioids are also known to affect seizure activity as well, opioids are looked in how they can be modulated in order to decrease seizure activity. Within the dentate gyrus (DG), there are two opioid peptides, enkephalins and dynorphins, which both have effects on excitability, but with contrasting effects (11). The difference between these two peptides is that enkephalins bind to delta- and mu- opioid receptors (DORs and MORs) whereas dynorphins bind to kappa-opioid receptors (KORs). However, unlike galanin receptors, opioid receptors can be activated by exogenous opiate drugs, which means that overdose can be possible because it is not reliant on an endogenous ligand. For example, the MOR agonist morphine can bind which means that a ligand can be introduced and not well regulated by the body, leading to overdose (11).

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Treatment-Resistant Postictal Agitation After Electroconvulsive Therapy (ECT) Controlled With Dexmedetomidine. The Journal of ECT. 2013;29(2):e18. O 'Brien, E., Rosenquist, P., Kimball, J., Dunn, G., Smith, B. and Arias, L. (2010). Dexmedetomidine and the Successful Management of Electroconvulsive Therapy Postictal Agitation.

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The drug culture swept through the nation encapsulating adults and juveniles to participate in the practice. However, reports about the damaging effects created mass hysteria and initiated the policies to restrict use. James L. Chapel and Daniel W. Taylor’s article, Drugs for Kick, discusses adolescent participation in drugs such as inhalants, narcotics (particularly marijuana), and hallucinogens (mainly LSD), as they examine effects, techniques, habits, clinical findings, association with crime, personality dynamics, treatment, and preventive measures. The article discusses one’s involvement with the drugs which can be supported by criminological theories. Chapel and Taylor did not explicitly state their hypothesis, subjects, methods, or results.

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Many medicines are mixtures of enantiomers. In the 1950s a new drug called thalidomide was introduced very successfully as a sedative. Doctors noticed that when it was prescribed to pregnat women, it eased the symptoms of morning sickness,, and so they used it in early pregnancy. However, by the late 1950s and through the 1960s, 12000 their limbs simply did not grow propely. Eventially it was realised that the cause of the problem was thalidomide the drug was affecting the foetuses of the pregnant

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MDMA also known as Ecstasy, is a synthetic, psychoactive hallucinogen. It creates feelings of increased energy, euphoria, and distortions in sensory and time perception. MDMA was initially popular amongst young adults, but now affects a wider span of users ranging from underaged children to older adults. MDMA is taken orally, usually as a capsule or tablet.

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In one of research paper titled, Basic and Clinical Studies of Endorphins she and her colleagues explore how endogenous produced opiate peptides influence addiction, pain, stress, and psychiatric illness. They reviewed, “possible cellular mechanisms for addiction, involvement of endorphins in the action of antipsychotic drugs, the role of endorphins in pain modulation, and studies of endorphins in normal subjects and psychiatric patients” (Bunney,1979 p.239). Many of her methods of conducting research in this field remain in use to this day. Through additional work she determined that the use of acupuncture that induced pain relief was due to the stimulation of beta-endorphin release, comparable to the bliss one receives from sex (Schwartz, 2013). Through these groundbreaking discoveries, she developed her own molecular theory of the emotions as bridging both mind and body.

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The etiology of PONV is multifactorial during laparoscopic cholecystectomy, therefore, combination of different classes of anti-emetics are preferred to control PONV, [6] [7] [205,206] including anticholinergics, antihistamines, butyrophenones, benzamide, dexamethasone and 5-HT3 antagonists. Ondansetron, 5- hydroxytryptamine type 3 (5-HT3) receptor antagonist, blocks receptors in the CTZ as well as vagal nerve terminals. Dexamethasone has been used as an anti-emetic for a long time with limited adverse effect. The exact anti-emetic mechanism of dexamethasone is unknown, but it is thought to enhance the anti-emetic effect of 5-HT3 receptor antagonists [8] [208] that is central/peripheral inhibition of production of 5-HT, central inhibition of synthesis of prostaglandins, changes in permeability of the blood brain barrier to plasma proteins, or by releasing endorphins.[9]

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Volatile anesthetics can alter the dopaminergic balance in the brain, but whether they exacerbate PD is unknown. Propofol produces both dyskinesias and ablation of resting tremor, suggesting that it has both excitatory and inhibitory effects in this patient population. But both volatile agents as well as propofol has been successfully to sedate patients with PD during deep brain stimulation surgery. Dexmeditomidine appears to be safe and when used in deep brain stimulation surgery has advantage of not interfering with motor symptoms. Ketamine should be used with caution because of potential interaction between levodopa and ketamine’s sympathomimetic activity.

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The hormone also has neurotransmitter functions in the central nervous system and peripheral hypertensive effects. Most vasopressin effects have been reported to be mediated through one of two receptors: the V1 and the V2 receptor (128). The osmoregulatory renal effects are exerted mainly via the V2 receptor, a 40 kD membrane-spanning protein located in the collecting ducts (129). Maximal antidiuresis is accomplished if 2.5% or more of the renal V2 receptor sites are occupied (130). On a cellular level, the activation of V2 receptors leads to the synthesis of cyclic adenosine monophosphate (cAMP), which, in turn, results in the translocation of intracellular aquaporin type 2 to the apical cell membrane (131, 132).

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[TORTORA]. The release of epinephrine and norepinephrine into the blood by the stimulation of the adrenal medulla. This is the mechanisms from the nerve impulse in the sympathetic nerves. The cellular metabolism is surged when the hormone in turn is bring back and increase the heat production. [TORTORA].

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