Pharmacology: Probitor, Cardiprin, Zocor, and Endone - Assignment Example

Pharmacology (Paramedic) Table of Contents Part 4 Question 4 Drug Probitor 4 Drug 2 - Cardiprin 4 Drug 3 - Zocor 5 Drug 4 - Endone 6 Drug 5 -Coversyl 7 Drug 6 (Lasix) 7 Drug 7 (Noten) 8 Drug 8 (Diaformin) 8 Part 2 9 Question 3 11 Question 4 11 Question 5 12 Question 6 14 Question 7 15 Question 8 16 Question 9 17 Question 10 18 a). 18 Question 11 20 Question 12 20 Question 13 21 Question 14 21 Question15. 22 Question16. 23 Question17. 24 References 25 Part 1 Question 1 Drug 1 - Probitor General Drug Name and Quantity: Probitor (20mg OD) Generic name of drug: Omeprazole (Massachusetts Medical Society, 2014) Drug class: Proton pump inhibitor (PPI) (State Government of Victoria, 2014) Approved indications: The quantified dosage of this drug finds wide applicability in treating multiple cases related to hyperacidity. In medical terms, this disorder is known as Gastroesophageal Reflux Disease (GERD). Certain associated symptoms of this disorder includes occurrence of inflation within the esophagus tube through which, food is delivered from mouth to stomach (Kefalas & Ciociola, 2011). In such cases, Probitor supports the appropriate treatment and works to prohibit further occurrence of such symptoms. Similar to this context, the utility of the drug also finds applicability for effective treatment of duodenal ulcer along with gastric ulcers. The spread of infection within the small intestine caused by Helicobacter pylori is one of the most prominent reasons of such ulcers. Related reasons include prolonged smoking and use of anti-inflammatory drugs (Kefalas & Ciociola, 2011). Drug Regulator: TGA approved (Kefalas & Ciociola, 2011). Drug 2 - Cardiprin General Drug Name and Quantity: Cardiprin (100mg OD) Generic name of drug: Acetylsalicylic Acid (Internationaldrugmart.com, 2014) Drug class: (Nonsteroidal anti-inflammatory drug NSAID) (Pountos & et.al., 2011). Approved indications: In medical practice, this drug finds wide applicability for treating viral fever and other forms of inflammations, which are often subjected to pain. Popular instances of such conditions can be addressed within individuals who might have been subjected to health related anomalies such as ‘arthritis’, ‘headache’, ‘strained muscles’, ‘migraine’ and ‘common cold’. The quantified dosage of this drug is highly effective in preventing major cardiac attacks and sudden strokes (Upfal, 2006, p. 51). Drug Regulator: The drug is manufactured by ‘Reckitt Benckiser (Australia) Pty Ltd.’, with the approval of Therapeutic Goods Administration (TGA) (Australian Government Department of Health and Ageingb, 2013). Drug 3 - Zocor General Drug Name and Quantity: Zocor (40mg OD) Generic name of drug: Simvastatin Drug class: statins (Rippe, 2011). Drug Class and Mechanism: The utility of this drug is specifically associated with the treatment of patients of high cholesterol. The working mechanism of this drug can be elaborated in a manner that it inhibits the secretion of enzymes within the human liver that in turn is responsible for the formation of cholesterol. Apart from being termed as Zocor, this drug also has an alternative name, i.e. HMG-CoA reductase inhibitor. In an associated manner, this drug also minimizes the level of Lipoprotein (LDL) that is termed as bad cholesterol within the human blood streams. Justification to this statement can be provided depending on the fact that excessive flow of high LDL dansified blood might result into multiple other forms of body anomalies, such as blockage within the coronary artery. In context to the lowering LDL density in blood, Zocor drug increases the percentage of High Density Lipoprotein (HDL) also termed as good cholesterol (Rippe, 2011). Drug Regulator: This drug received a comprehensive approval from The US Food and Drug Administration (FDA) as on 1991 (Rippe, 2011). Drug 4 - Endone General Drug Name and Quantity: Endone (5mg PRN) Generic name of drug: Oxycodone Hydrochloride (Beck 2001, p. 604). Drug Class and Mechanism: Endone (5mg PRN) is a form of a pain reliever drug that is prescribed by the doctors to those patients who may or may not have any narcotic addiction. In addition to this drug, multiple non-narcotic pain relieving drugs are also prescribed, taking due consideration of the fact that prolonged usage of the Endone drug might turn out to be an addiction. Considering its mechanism, it can be stated that this drug, upon consumption, secrets a chemical compound termed as Opioids, which is effective enough in countering pain occurrence within the body. As an active mechanism, the Opioids secreted by the Endone drug also intercepts the neural transmission of pain signals and thus, improvises the Behavioral patterns of the human body towards painful sensations. Apart from the bright part, the prolonged consumption of this drug might result in multiple other forms of body functionality disorders, such as excessive sleepiness and breathing issues (Beck 2001, p. 604). Drug Regulator: TGA approved (Beck 2001, p. 604). Drug 5 - Coversyl General Drug Name and Quantity: Coversyl (5mg OD) Generic name of drug: Perindopril (Nicholson, 2007, p. 148). Drug Class and Mechanism: This drug belongs from three main classes namely Antihypertensive, Renal Protective Agent and Cardiovascular Agent. The utility of this drug finds effective applicability for treating patients who are subjected to high blood pressure. It also acts as a preventive measure against cardiac arrest. The mechanism associated with this drug can be elaborated in a manner that it releases angiotensin-converting enzyme upon consumption that inhibits the retention of salt and other fluid forms within the human body, which in turn is responsible for increasing pressure on normal blood flow and heart functioning (Nicholson, 2007, p. 148). Drug Regulator: TGA Approved (Nicholson, 2007, p. 148). Drug 6 (Lasix) General Drug Name and Quantity: Lasix (40mg OD) Generic name of drug: Frusemide Drug Class and Mechanism: This drug belongs from the diuretic class and is utilized for reducing the liquid pressure within the human body. Such lasting tenure of this drug is approximately 100 minutes and is prescribed by doctors in case of electrolyte instability within the human body. It regulates the level of Sodium chloride in the human kidneys and helps in draining out the excessive fluid to stabilize the blood pressure (Niblett, 2006, p. 95). Drug Regulator: FDA Approved (S4 scheduled) (Niblett, 2006, p. 95). Drug 7 (Noten) General Drug Name and Quantity: Noten (50mg OD) Generic name of drug: Atenolol (Tizian, 2013, p. 175). Drug Class: Beta-blocker (Tsalta & et. al., 2008) Mechanism: In medical science, this drug is used for treating pain related disorders such as ‘myocardial infarction’, ‘hypertension’, ‘angina’ and ‘migraine’. This drug releases effective antihypertensive enzymes to block the excessive production of ‘antihypertensive’ ensuring proper cardiac functioning without much reflexive changes in the ‘peripheral vascular resistance’. Moreover, prolonged usage of this drug might result in multiple other disorders such as fatigue, instability within other enzyme metabolism, hallucinations and multiple more (Tizian, 2013, p. 175). Drug Regulator: TGA Approved (S4 scheduled) Drug 8 (Diaformin) General Drug Name and Quantity: Diaformin (850mg BD) Generic name of drug: Metformin hydrochloride (Hamilton, 2011, p. 162). Drug Class and Mechanism: This drug is prescribed to those patients who are subjected to type-2 diabetes. Diaformin mainly targets the absorption and secretion of glucose within the human body and keeps it in balanced proportion that will be required by the diabetic patient. It also produces certain chemical enzymes that inhibit the absorption of excessive glucose by the human muscle tissues (Hamilton, 2011, p. 162). Drug Regulator: TGA Approved (S4 Schedule) (Hamilton, 2011, p. 162). Part 2 Question 2 Medicine 1: Blackmores Joint Formula (OD) Active Ingredients Glucosamine (942mg within the overall mixture ) Chondroitin Sulphate Sodium (250mg) Manganese (8.8 mg) Boron (8.8 mg) Dosage- Regular dosage includes consumption of one tablet /day Source: (Nash &et. al., 2014) Medicine 2: Natures Way Brain and Memory supplement (OD) Active Ingredients Fish oil natural (1000mg) Eicosapentaenoic acid (EPA) (180mg) Docosahexaenoic acid (DHA) (120mg) Pyridoxine hydrochloride (Vit B6) (10mg) Glutamine (100mg) Folic acid (100mcg) Cyanocobalamin (Vit B12) (100mcg) Ginkgo dry leaf (3000mg) Ginkgo flavonglycosides (14.4mg) Ginkgolides along with Bilobalide (3.6mg) Dosage- Regular dosage includes consumption of one tablet /day Source: (Natures Way, 2014) Medicine 3 - Blackmores Mood Support St Johns Wort supplement (OD) Active Ingredients Hypericum perforatum (1.8g) Dosage- Regular dosage includes consumption of one tablet /day Source: (Blackmores Australia, 2014) Question 3 a) Journal: Staines & Therapeutics, (2011) Type of interaction: pharmacodynamic Mechanism of interaction: drug-to-drug interaction Clinical consequences of the interaction: chest pain, nauseous feeling, difficulty in breathing b) Information source: anecdotal report Strength factors Indication of the negative consequences of drug interaction with the herbal components of the previously consumed drug Possible signs and causes of mood disorder and feeling of congestion within the chest Possible changes increasing body and organ toxicity Source: (Staines & Therapeutics, 2011) Question 4 Provided Drug Name- Frusemide Effective against- Prevention of excessive water retention within the body Provided Patient Issues: chest congestion, ‘nauseous feeling in stomach’ Mechanism of action: - The frusemide drug belongs to the diuretic class of medicine, which inhibits the excessive absorption of salt within the human body, and in turn is responsible for imparting additive pressure within the blood vessels. It is prescribed to patients who are subjected to issues related to heart congestion or kidney malfunction. These factors find specific alignment with the provided cases where Howard has stated about his subjection to chest congestion (Ronco &et. al., 2008, p. 853). Majority of the elemental minerals and sodium chloride is filtered out by the kidney upon passage. Accordingly, the filtered molecules are mixed with the urine and are eliminated out of the body. However, normal human body projects the behaviour of reabsorbing those filtered mineral molecules before they are mixed up with the urine. At this point, the frusemide drug prohibits the re-absorption of the filtered molecules by the body and passes them out as urine. However, prescription of this drug should be carried out under proper supervision of the doctors, failure to which might result in loss of essential minerals from the human body (Ronco &et. al., 2008, p. 853). Thus, prescribing this drug to Howard might help in reducing his chest congestion problem by regulating the percentage of sodium chloride within his body. Question 5 Article 1: Pickkers et al. (2014) Type of study: Randomized Control Trial Comparator: ‘direct arterial vasoactivity’, ‘norepinephrine-induced vasoconstriction’ Sample size: n=22 Measures of efficacy: Blood pressure, hemodynamic changes Key results: No signs of change in ‘blood pressure, FBF and heart beat rate’ got recorded in case of ‘infusing frusemide’ into the body through ‘arterial vasoactivity experiment Increase with blood pressure observed from ‘113±2/62±1 to 116±2/66±2 mm Hg’ within one hour in case of ‘venous vasoactivity experiment’ The increase or decrease depends on the quantity of frusemide being injected in the body No such change in the heart beat rate was recorded after the frusemide being administered Source: (Pickkers et al., 2014) Critique: Strengths: Due to the randomized sequence, the results obtained from the study can be considered effective in order to understand the regulatory impacts of frusemide on blood pressure of a human body Pickkers et al. (2014) Weaknesses: The conducted medication study has been ineffective for understanding the reasons as to why both the techniques of infusing frusemide into the body did not bring about any change in the heart rate. The entire study contradicts to the usage of this drug for treating heart congestions (Pickkers et al., 2014). Article 2: Ho & Sheridan (2006) Type of study: Randomized control trial Comparator: Ototoxicity rate Sample size: n=849 (having or without the risk of renal disorder) Measures of efficacy: total percentage of test subjects cured Key results: No significant changes have been witnessed in the count of test subjects suffering from renal disorder Increased signs of deafness has been recorded within patients infused with higher concentration of frusemide Relative signs of Tinnitus occurrence also got recorded within the patients Critique: The conducted study has been highly informative regarding the positive impact of infusing frusemide into patients subjected to renal disorder. The data used for this analysis has been collected from previously existing records. The comparison made between the one time user of frusemide drug with that of the prolonged drug user have laid down credential data about the momentary and prolonged changes within the body because of frusemide drug utility. However, for the downside, it can be stated that the study did not turn out to be that effective towards finding an alternative solution through which, the effectives of frusemide drug can be enhanced (Ho & Sheridan, 2006). Question 6 Article 1: Nieminen et al. (2005) Type of study: anecdotal report Comparator agent: isosorbide dinitrate Sample Size: n=0 Measures of effectiveness: reduction of mortality rate associated with heart failures Key results: Infusion of GTN drug within patients has proven to be highly effective in minimizing the mortality rate by appreciable count The presence of nitrate element within this drug proves to be beneficial in dilating and widening the blood carrying arteries and minimizing the blood pressure Source (Nieminen & et al., 2005) Article 2: Sen et al. (2013) Type of study: anecdotal report Comparator agent: Tramadol Sample Size: n=0 Measures of effectiveness: Reduction of mortality rate Key findings: GTN positively supports the antoxidative effect on the patient’s body Negative impacts of GTN infusion within animals Source (Sen & et al., 2013) Question 7 a). Identified factors: Previous recorded heart rate, present heart rate, blood pressure, breathing rate. b). GTN (Glyceryl Trinitrate) is a nitrate agent that supports the fluidity of the human heart. In order to accomplish that, this agent releases appropriate enzymes that minimize blood density and promotes greater blood flow through the arteries. In a comprehensive manner, without prior checkup, the utility of this drug might result in excessive bleeding from exterior organs (Rathbone & et. al., 2002, p. 375). c) Risk benefit relationship (Rathbone & et. al., 2002, p. 375) Fluidity within blood flow will keep the heart under normal pressure avoiding possible signs of failure Effective breathing rate will ensure minimized pressure on the body d) Strategies for addressing factors (Rathbone & et. al., 2002, p. 375) Appropriate monitoring and infusion of balanced dosage of GTN Constant monitoring of the rate of platelet aggravation that might be a sign of STEMI Monitoring of the pressure and the count on the heart beat rate. Question 8 a). Article 1. Tran et al. (2000) Study type: anecdotal report Study duration- 2 to 3 days Sample size: n= 865000 Outcome measures: Clopidogrel along aspirin can be utilized as an effective therapative technique through which the formation of blood clot as a result of platelet aggregation can be minimized through long term treatment (Tran &et al., 2000). Article 2. Zeymer &et al. (2006) Study type: Anecdotal report Study duration: nil Sample Size: nil Outcome measures: This journal also projected the beneficiary aspects associated with utilizing aspirin as a remedial treatment against STEMI patients. Projected data elaborates the effectiveness of Stemi in minimizing the platelet aggregationand blocking of all the ‘thromboxane-mediated’ pathways that lead to intensive bleeding (Zeymer & et al., 2006). B). The overall outcomes of administering aspirin within patients suffering from STEMI has proved to be highly beneficial in terms of minimizing the mortality rate by appreciable rates. However, the mandate factors require the conduction of prolonged treatment. Question 9 A). Assuming the scenario, where the patient has been witnessing heartache due to increased blood pressure and formation of blood clots within the artery walls. Possible blockage within the artery walls can be considered as possible reasons for such pain occurrence (Zeymer & et al., 2006). B). Clopidogrel undergoes drug-to-drug interaction with multiple other forms of blood thinners, such as Dilantin or Ticlid that is prescribed with it to minimize the density as well as the formation of blood clots within the artery walls. Eventually, it minimizes the excessive pressure building up within the blood arteries that might lead to heart failures (Aschenbrenner & Venable, 2009, p. 610). Question 10 a). Type of interaction: Drug to drug Mechanism of interaction: Continued usage of Blackmores Mood Support St Johns Wort supplement (OD) medicine has resulted in giving rise to multiple forms of mood disorders. The associated symptoms also include cardiac pain, nostalgic feeling and breathing problem. In such context, the blood thickening and cot prevention mechanism of clopidogrel appears effective in minimizing the pressure on the heart and blood flow (Jewell & Blackmore, 2004, p. 70). Clinical consequences of the interaction Decreasing efficiency of clopidogrel drug Increased pressure on the blood arteries and the heart Risk of heart failure and breathing problem b ) . Genuinity of the evidence Type of report - anecdotal report Strengths – 1. Highly detailed in terms of providing clinical consequence explanations 2. Impartment of knowledge regarding drug interaction Weaknesses – 1. Absence of information regarding chemical and molecular interaction Source (Drugs.com.b, 2014) Part 3 Question 11 A). Percentage bonding of Metformin with the plasma protein: (negligible i.e. > 5.0 Percentage (Spratto & Woods, 2011, 1944). B). Taking consideration of the fact that Metformin does not bind with the neighbouring blood plasma, its unbound fraction i.e.( fu) always gets assumed as 1(Eyal et al., 2010). C). From the pharmacological perspective it can be stated that subsequent alteration of the concentration of plasma albumin does bring about significant changes in the protein binding of Metformin drug. Moreover, increasing the concentration of plasma albumin substantially elevates the protein binding factor and thus, the rental clearance factor associated with the drug associatively falls (Pharmacol, 1992). Question 12 A). The volume of distribution (Vd) of Metformin drug is approximately 654 L (Flomenbaum, 2006, p. 166). B). The absorption level of this drug subsequently depends on the effective body circulatory system which in turn depends on the blood volume. As an associated result, the distribution pattern of this drug will be large in relation to the blood volume (Flomenbaum, 2006, p. 166). . C). The volume distribution of Metformin comprises of 850 mg of dosage (654 + 358 L.). The chemical composition of this drug restricts its bondage with the plasma protein. However, the ‘steady state plasma concentration’ associated with this drug varies depending on whether it gets provided as normal clinical dosage (c 1 pg/mL) or as controlled clinical trials (5 ug/mL) (Flomenbaum, 2006, p. 166). Question 13 A).The identified fraction excreted unchanged in urine (fe), associated with the intake of Metformin drug has been found to be (>0.5) (Department of Clinical Pharmacology, 2014). B). Percentage excreted as metabolites- (90 to 100) percentage (American Academy of Family Physicians, 2014) Question 14 A). Drug absorption organs: Stomach (apical membrane, intestinal cells, basolateral membrane), blood carrying arteries and veins, heart, liver, kidneys, peritubular capillaries, renal veins, Bowman’s capsule B). The reaction type associated with the circulation and elimination of Metformin elimination from the body can be stated as functional. Moreover, the below provided diagram elaborates about the circulation procedure of this drug through the targeted organs (Faqi, 2012, p. 12). Source: (PharmGKB, 2014) C). Types of enzymes and transporters involved - Transporter: OCT2 Gene: SLC22A6 Source: (Faqi, 2012, p. 12) Question15. Determination of systemic clearance: A). Q (Normal hepatic blood flow within Humans) (21) Clint (‘intrinsic capacity of the hepatocytes to metabolize a drug’) (2.63+/- 0.48) ~ 2.63 F (fraction of free drug) 6.54 Hepatic Clearance: Cl (h) = Q [(f x Clint) / (Q+ f x Clint)] = 21[(6.54*2.63) / (21+6.54*2.63)] = 9.455 Urine concentration (Cu): 25mmol/L Urine flow rate (Q): 120ml/min Plasma concentration (CB): 0.45mmol/L K (renal clearance) = (Cu*Q)/CB = 6.66666.66 [L/min] (McCrory, 1979) B). Clearance classification of Metformin: High Renal Clearance C). Taking consideration of the clearance equations and the clearance classification of Metformin, it can be stated that clearance deterrents such as unbound fraction, secretion and renal vein re-absorption are crucial factors that help in enhancing the effectiveness of this drug. Question16. A). Oral bioavailability of Metformin: 50-60 % (Vogel &et. al., 2010, p. 283). B). The bioavailibity of a drug specifically depends on its Gastrointestinal (GI) absorption rate. In medical terms, appropriate absorption of the drug by the GI tract subsequently increases the effectiveness of the metformin drug. Similarly, the effectiveness of the metformin drug also gets tremendously reduces because of the ‘first pass hepatic extraction’, due to the fact that this metabolism reduces the necessary concentration of metformin in the liver itself before it gets to the body circulatory system (Vogel &et. al., 2010, p. 283). C). Bioavailability of the metformin drug might increase in case it gets effectively absorbed by the gastrointestinal tract. However, the contrary case might happen in situation if it is subjected to ‘first pass hepatic extraction’ (Vogel &et. al., 2010, p. 283). Question17. The clearance factor of the metformin drug does not appear to alter much on being subjected to environmental factors, such as smoking or drinking. However, the disease state of the patient might directly hamper the clearance rate of the drug taking consideration of the fact that drug clearance majorly depends on the appropriate functioning of the liver and the kidneys (renal clearance) (Vogel &et. al., 2010, p. 283). Question18. Based on the understanding of pharmacokinetics of metformin, it can be stated that one should continue using this drug with appropriate dosage. The intention is to regulate the concentration of this drug when passed through ‘first pass hepatic extraction’. Moreover, an appropriate dosage will also ensure effective absorption of this drug by the gastrointestinal tract, which in turn helps in enhancing the curability factor of this drug by considerable percentage (Vogel &et. al., 2010, p. 283). References Australian Government Department of Health, 2003. Fluticasone and Adrenal Crisis. The Glitazones - Early Experience. 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Effect Of Clopidogrel On 1-Year Mortality In Hospital Survivors of Acute ST-Segment Elevation Myocardial Infarction in Clinical Practice. European Heart Journal, pp. 1-6. Read More