Agonist-Induced Desensitization Case Study

In psychotherapy there are many different ways that a therapist can decide how to treat a client. In my paper I will discuss how Exposure Therapy and Behavioral Therapy work together with a client. I will focus on the nature of the problem, the process of change, theory in practice, multicultural considerations, and the types of clients and clinical problems.

Pharmacodynamic and pharmacokinetic differences inhibit this variability of response. Pharmacodynamics show how a drug affects the body, considering that, pharmacokinetics describes how the body revises the drug. Pharmacokinetics assist the variability feedback to narcotics by affecting the availability of a drug. The manufacturing of active or inactive metabolites, and their eradication from the body. Pharmacodynamic factors contributing to the variability of response to opioids include between-patient differences in specific opioid receptors. The intention of drug retention is for the narcotic to travel in the blood, and the goal is for it to circulate in the brain. The substantia nigra and the ventral tegmental summons the brain that a narcotic is being used which causes dopamine throughout the body. “The brain is naturally inclined to learn to want to repeat actions that stimulate the reward system or provoke feelings of pleasure. Of course without opiates, the actions your brain wants to repeat are things like sex or eating. Once you’ve taken opiates, your brain starts to want to repeat that activity, and that’s how addiction develops”

Dopamine receptors are g-protein coupled receptors (GPCRs) which exist in two families of subtypes. Activation of D1-like receptors (D1 and D5) induce adenylyl cyclase activity which increases levels of cAMP and subsequent PKA activation. Conversely, D2-like receptors (D2, D3 and D4) inhibits production of cAMP and subsequently reduces PKA activation (Beaulieu J-M and Gainetdinov RR, 2011).

In the urine storage phase, the bladder is passively filled and subjected to low pressure. In contrast, for micturition, coordination of detrusor contraction is required with the relaxation of the internal and external urinary sphincter. To achieve this normal urination with urinary continence, control by the central nervous system, which coordinates the activation of the sympathetic and parasympathetic nervous system with the somatic nervous system, is required. Therefore, damage or diseases of the central, peripheral and autonomic nervous system can lead to neurogenic bladder dysfunction.

For instance, the ability of THC and the synthetic CB1 receptor high efficacy agonist CP 55,940 to produce a positive place preference in rats and mice has been shown to depend on the timing of injections as well as on the range of doses used (Lepore et al. 1995; Valjent and 2000; Braida et al. 2001; Ghozland et al. 2002) as it does with other drugs (Bardo and Bevins 2000; Tzschentke 1998). Lepore et al. (1995) demonstrated that when a standard schedule of daily injections (i.e., vehicle, drug, vehicle, drug, etc.) before consecutive daily sessions was used, THC produced a conditioned place aversion for the compartment associated with its administration at a low 1.0 mg/kg dose but positive place preferences at higher 2.0 and 4.0 mg/kg doses. When the schedule of daily injections was changed, allowing a longer wash-out time period between drug injections (i.e., vehicle, day off, drug, day off, vehicle, day off, drug, etc.), THC produced a conditioned place preference at a low 1.0 mg/kg dose but produced place aversions at higher 2.0 and 4.0 mg/kg doses. The authors suggested that increasing the interval of time between THC injections might qualitatively change the effects of THC in this behavioral test, due to a “postdrug dysphoric rebound.” This may help to explain the

Albuterol acts on beta2-adrenergic receptors located in the smooth muscle of respiratory tract. Activation of beta-2 receptors results in subsequent increase in adenyl cyclase and cyclic AMP. Increase in cyclic AMP leads to the activation of protein kinase A, inhibiting phosphorylation of myosin, thereby lowering intracellular ionic calcium concentrations, resulting in relaxation of the smooth muscle

This week I learnt about chlorpromazine, which is an antipsychotic. It is also used in short-term management of anxiety, agitation or disturbed behaviour in non-psychotic disorders. Chlorpromazine is an antagonist of many receptors, which include α1 adrenoceptor, M3 muscarinic receptor, H1 Histamine receptor, 5HT2 receptor, dopamine D2 receptor and angiotensin II AT1 receptor. This illustrates one of the pharmacology principles, which is selectivity of a drug. A highly selective drug (‘clean drug’) binds to only one receptor or molecular target whereas a drug having low selectivity (‘dirty drug’) will bind to many targets in the body. Binding upon many receptors can produce many effects but some effects are not desired. For example, chlorpromazine

Ms. Jones is in an extremely critical situation, due to her development of cardiogenic shock and her current need for multiple catecholamines. Cardiogenic shock is the end result of substantial cardiovascular injury with myocardial infarction and emergent revascularization being at the top of the list (Levy et. al, 2015). Patients that experience cardiogenic shock need extensive care and monitoring which has landed her a place on the critical care unit. Dopamine has predominantly beta-adrenergic effects at lower doses and alpha-adrenergic effects at higher doses, but its effects are relatively weak (Vincent & Backer, 2013). If the dopamine and dobutamine used reach their therapeutic maximums, the physician may consider adding other Alpha and

In vitro: Previous study indicated that both CID-2745687 and ML-145 could competitively inhibit the effects of cromolyn disodium and zaprinast (two agonists sharing an overlapping binding site) on human GPR35. In contrast, though ML-145 antagonized the effects of pamoate competitively, CID-2745687 showed a noncompetitive fashion. Additionally, neither ML-145 nor CID-2745687 was able to antagonize the agonist effects at rodent ortholog of GPR35 [1].

Disulfiram (Antabuse) is used to treat alcoholism in conjunction with other treatments such as counseling. Disulifirams mechanism of action is that it creates sensitivity to alcohol that can be very unpleasant to the patient if any amount of alcohol is ingested. It blocks the oxidation of alcohol at the oacetaldehyde stage. It increases the concentration of acetaldehyde during the alcohols metabolism by 5 to 10 times higher than without the Disulfiram. This increased metabolism causes the very unpleasant symptoms associated with this therapy hopefully resulting in aversion therapy.

Adrenoceptors have a specific structure which allows a drug or hormone to bind to it. They are found in the heart, blood vessels and the lungs and can be stimulated by catecholamine binding, thus increasing the activity of the cell in the body. There are two types of adrenoceptors, alpha (α) and beta (β) and these have subclasses α₁, α₂, β₁, β₂, and β₃ (Burnstock and Verkhartsky., 2010)

Anti-muscarinics and antispasmodics agents fall under the autonomic-anticholinergic classification type of medication. Anticholinergic medications have similar pathologies, though they are used for different medical conditions such as overactive bladder, irritable bowel syndrome, Parkinson’s disease and certain psychological issues to name a few. The pathology of these medications is through by binding of the neurotransmitter acetylcholine, blocking of the parasympathetic ability to bind the target receptor. According to Williams & Baer (1998), anticholinergic drugs such as, anti-muscarinics and antispasmodics, interrupt parasympathetic nerve impulses by competing with the neurotransmitter acetylcholine at muscarinic receptor sites, this

The physiological function of each receptor subtype has not been established and is currently the subject of intensive investigation (1).

G-protein-coupled receptors (GPCRs) are a large family of membrane proteins that mediate our physiological responses to hormones, neurotransmitter, and environmental stimulants. Therefore, they have great potential as therapeutic markers for a wide range of diseases. Arena’s purpose in this respect, is to exploit their potential to strengthen the well-being of patients,

These specialists intensely and explicitly tie to the M3 receptor subtype more than other muscarinic receptor subtypes, except for tolterodine, which has exhibited no specificity for any subtype.