PHARMACOLOGY BLOCK 2 : CNS & PAIN

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university PHARMACOLOGY 214202 Fichas sobre PHARMACOLOGY BLOCK 2 : CNS & PAIN, creado por wallacejr@hotmail.co el 10/08/2015.
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Pregunta Respuesta
1. Identify 6 principal chemical transmitters involved in brain function and the functions they influence. norepinephrine (noradrenaline); Arousal, sleep, mood, appetite, hormone release,body temperature. dopamine; Skeletal muscle movement, behaviour, emesis, hormone release. acetylcholine; Cognition, skeletal muscle movement, memory,consciousness 5-hydroxytryptamine (5-HT, Serotonin); As for NE plus behaviour, pain transmission, emesis. gamma-amino butyric acid (GABA); Motor control, memory, consciousness.GABAA is associated with the chloride ion channel and GABAB is associated with the calcium and potassium channels. glutamate (an excitatory amino acid); (EAA) which is found in all regions of the brain and possible illnesses associated with glutamate are Alzheimers, Huntingtons, epilepsy, and stroke. Opioids; are also very important neurotransmitters in the brain. Opioid receptors are present in the CNS as well as in the body. Section 2.9 fully explores the effects of having opioid receptors in the CNS.
2. Identify some illnesses that are based on alterations in neurotransmitters in the brain. Noradrenaline; Depression, insomnia, eating disorders, narcolepsy, ADD Dopamine; Parkinson’s disease, schizophrenia, aberrant behavior, psychoses 5-hydroxytryptamine (5-HT, Serotonin); Depression, ADD, headaches, eating disorders, insomnia, Acetylcholine; Parkinson’s disease, dementia. GABA: Anxiety, insomnia, aberrant behaviour, epilepsy.
3. Identify where drugs can be designed to work in the chemicaltransmitter- receptor systems. A. Drugs can be designed to enhance the activity of a neurotransmitter by acting on different areas of the neurotransmission pathway. For example:  Drugs can be agonists and mimic the neurotransmitter.  Drugs can be precursors for the neurotransmitter.  Drugs can inhibit the neurotransmitter from being broken down.  Drugs can inhibit the reuptake of the neurotransmitter. The above type of drugs will ensure there is a neurotransmitter (or something that mimics the neurotransmitter) present to bind to its receptor and carry out the associated function. These drugs are used when the disease is a result of too little neurotransmission, e.g. depression, Parkinsons. B. Drugs can be designed to block the neurotransmitter’s action or response. For example:  Drugs can be blockers or antagonists and hence stop the neurotransmitter from binding to the specific receptor.  Drugs can enhance the action of the inhibitory transmitters, such as GABA, or inhibit the action or release of the exciteatory amino acids such as glutamate. These drugs ARE A RESULT OF TOO MUCH neurotransmittion
neurotransmission disease is too much- seizure disorders to little- depression
1. Which neurotransmitters are involved in the following functions? (a) mood (b) vomiting (c) memory (d) skeletal muscle movement 1. (a) NE and serotonin (b) dopamine and serotonin (c) acetylcholine and GABA (d) dopamine and acetylcholine and GABA
2. State which neurotransmitters are involved in the following conditions. State whether there is too much neurotransmitter or too little and then explain how drugs could be used to help in the treatment of the condition (a) depression (b) psychotic episodes (c) Parkinsons 2. (a) Low levels or activity of NE and serotonin. Drugs used to enhance the levels or activity of NE and serotonin. (b) High dopaminergic activity. Drugs used to inhibit the dopaminergic nerve response. (c) Imbalance in dopamine and acetylcholine neurotransmitters. Low activity of dopamine and high activity of acetylcholine. Drugs used to enhance dopamine levels or dopaminergic activity and decrease acetylcholine activity.
psychosis is neurosis is Psychosis is defined as disordered thinking and disturbed emotional tone. Psychosis is a symptom not a disease. Neurosis is defined as thinking patterns which are basically normal but disturbed emotional tone.
discuss the appropriate use, mechanism of action and adverse effects of antipsychotic drugs and identify key concerns with their use. Compare and contrast the typical and atypical antipsychotics as regards drug action and adverse effects.
Compare and contrast the typical and atypical antipsychotics as regards drug action, onset, and adverse effects. MODE OF ACTION UNKNOWN BUT Dopaine receptor–blocking activity in the brain: All of the first generation and Most of the second- generation antipsychotic drugs block dopamine receptors in the brain and the periphery (except Clozapine- like atypical). – ONSET The clinical efficacy of the typical antipsychotic drugs correlates closely with their relative ability to block D2 receptors in the mesolimbic system of the brain ADVERSE; OLD::OLD::• Extrapyramidal effects ADOPT (Akathisia (restless) Dystonia (spams) Oculogyric ( rolling eye) Parkinsonism (tremors) Tardive (unreversiable ticks) ) • Postural hypotension • Anticholinergic • Sedation • Weight gain • Endocrine effects ‐ e.g. hyperprolactinaemia • Neuroleptic Malignant Syndrome (NMS) ATYPICAL: • Weight gain, dyslipidaemia‐ increased risk of CVD • Diabetes type 2 ‐ especially with Clozapine and Olanzapine‐ due to insulin antagonist effect – impair glucose entry into cells + impair lipolysis in adipose tissue • Therefore –assess risk factors for metabolic syndrome etc, family history, monitor‐ blood tests •
The therapeutic effects of antispychotic drugs are believed to be due to reduced transmission/ action of which neurotransmitter? 1. Dopamine.
Read the article: Pollard, A., Friedman, T. & Aslam, M. (1994). Tranquillising actions. Nursing Times, 90 (11), 34-36, and answer the following questions. 2. (a) Tardive dyskinesia is an EPS of some antipsychotic drugs. When would you see this adverse effect develop? (b) How can the risk of tardive dyskinesia be minimised? (c) Skin reactions are a common problem with phenothiazines, and chlorpromazine in particular. What would you advise the patient if they are taking chlorpromazine? (d) If a patient is taking Clozapine, what must be done regularly to ensure that the drug is not toxic to the person? 2. (a) Tardive dyskinesia is a long-term adverse effect that does not normally develop until after several years of taking antipsychotics. (b) The risk can be lessened by using only the minimum amount of medication necessary and if possible, choose an antipsychotic that does not have EPS adverse effects as a major factor. (c) That they are susceptible to sunburn so when they go out it is important to protect their skin e.g. cover it up and use high protection sunscreen. (d) Must receive weekly blood tests because agranulocytosis is an adverse effect.
3. One of the adverse effects of antipsychotic drugs is parkinsonism. Explain why this occurs. 3. Antipsychotics are dopamine antagonists which means they block the effects of the neurotransmitter dopamine. Low levels of dopamine stimulation causes parkinsonism.
Read the article: Gray, R. (2001). Medication for schizophrenia. Nursing Times, 97 (31), 38-39, and answer the following questions. 4. (a) Name the typical and atypical drugs. (b) Explain the difference between typical antipsychotics and atypical antipsychotics? 4. (a) Examples of drugs which are known as typical or conventional antipsychotics are Haliperidol, Fluphenazine decanoate (Modecate) and Chlorpromazine. Examples of atypical antipsychotic drugs are Risperidone, Olanzapine, and Clozapine. (b) There are marked differences between atypical and typical antipsychotic drugs. Typical antipsychotics are referred to as the conventional or older antipsychotic drugs. 50% of patients treated with typical antipsychotics develop extrapyramidal adverse effects (EPS). These drugs may also cause other adverse effects, including sexual dysfunction, weight gain and sedation. These drugs may also cause cardiac arrythmias. Atypical antipsychotics are the newer antipsychotic drugs. These antipsychotics have fewer adverse effects and are not implicated in the development of EPS symptoms. Atypical antipsychotics are not free from adverse effects but, overall, treatment with these drugs produces a dramatic reduction in their appearance. This is one of the main reasons for their increasing popularity. Atypical antipsychotics may also be more useful in treati
Read the article: Buist, A. (1998, April). Understanding postpartum psychiatric disorders. New Ethicals Journal, 43, 46-47, and answer the following questions. 5. (a) What are the presenting symptoms for postpartum psychosis and when do they occur? (b) What is the pharmacological treatment for postpartum psychosis? (c) Do psychotropic medications pass into breastmilk? What are the implications? (d) Why should Lithium be avoided? 5. (a) mood swings, and involve a manic phase followed by depression. This is quite similar to symptoms in bipolar depression. high anxiety. confusion and delirium. rapid onset, and occur in the first week postpartum. (b) the same for other psychotic illnesses. The drug choice is dependent on the particular situation. Antidepressants are also used for treatment. Many women suffering from puerperal psychosis require A antidepressant and antipsychotic. early intervention (c) Yes THEY cross over into the breastmilk. reports of toxicity accumulation in infants. CAUTION IN premature babies.as THEY have a decreased ability to deal with the effects of the drug. no actual evidence that psychotropic drug treatment will cause long term harm to an BABY. (d) Lithium is excreted into breast milk and toxic symptoms at a lower concentration in the infant.Long term Lithium may MESS WITH infant’s kidneys and thyroid
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