Your assignment is just a click away

We have the best writers

We guarantee you plagiarism free, well formatted, grad A+ papers!

Drug Pharmacology and Pharmacokinetics

Drug Pharmacology and Pharmacokinetics

QUESTION
1. Drug pharmacology, pharmacokinetics
2. Brand name
3. Generic name
4. Dosing
5. Indications for use
6. Side effects
7. Contraindications
8. Pregnancy class
9. Cost analysis of the drug.
10. Provide a patient case study on a patient in which you would utilize sumatriptan and include at least two peer-reviewed evidence-based studies related to the drug.
11. Describe the appropriate patient education.
12. What is your role as a Nurse Practitioner in prescribing this medication
13. Describe the monitoring and follow-up.

Drug Pharmacology and Pharmacokinetics
ANSWER

Sumatriptan is in a class of drugs called triptans or selective serotonin receptor agonists (NHS, 2019). It works by constricting cranial blood vessels, blocking the release of neuropeptides that cause inflammation, and blocking the release of certain substances that cause pain, nausea, and other symptoms of migraines.
Sumatriptan is an agonist of 5-HT1B and 5-HT1D that leads to the narrowing of cranial blood vessels and inhibition of inflammatory peptides. Sumatriptan decreases blood flow to the carotid artery but increases the velocity in the internal carotid artery and middle cerebral artery. A migraine causes blood vessels in the brain to expand and releases chemicals responsible for nausea, swelling, and irritation (NHS, 2019). Sumatriptan works by negating the symptoms caused by migraines
The pharmacokinetics differs depending on the route of administration.
Absorption
A 6mg subcutaneous injection reaches a maximum serum concentration of 69.5 ng/ml, which translates to 95% within twenty minutes of administration (“Sumatriptan,” 2022). It has a bioavailability of 100%.
A 25mg oral dose reaches a maximum serum concentration of 16.5ng/ml, which translates to 95% within an hour and a half of administration (“Sumatriptan,” 2022). It also has a bioavailability of 14.3%.
A 20mg nasal spray reaches a maximum serum concentration of 12.9 ng/ml, which translates to 15.8%. It also has a bioavailability of 15.8%.
The volume of distribution: Sumatriptan has a volume of distribution of 2.4L/kg.
Protein binding: Sumatriptan binds to proteins by 14-21% in circulation.
Metabolism: Sumatriptan is metabolized by hepatic monoamine oxidase A isoenzyme to release its main metabolites; inactive indole acetic acid and indole acetic acid glucuronide.
Elimination route: Approximately 22% of Sumatriptan is excreted in the urine as unchanged Sumatriptan, approximately 38% as indole acetic acid in the urine, and approximately 40% of Sumatriptan is excreted through feces.
Half-life: Subcutaneous Sumatriptan has a half-life of 1.9h, oral 1.7h, and nasal 1.8h.
Clearance: Intravenous Sumatriptan has a clearance of 0.22L/min, oral 0.17L/min, and intranasal 0.21L/min. Overall, total plasma clearance is roughly 1200ml/min.
Pharmacogenomics effects: Researchers have directly studied Sumatriptan interaction with guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3, genotypes (C; T) / (T; T), T allele and found that patients with this genotype have an increased likelihood of responding to Sumatriptan, especially when treating cluster headache.
Food interactions: Take Sumatriptan with food and water. When taken with Sumatriptan, chronic alcohol consumption increases the risk of gastrointestinal bleeding, ulcers, and perforations.
Toxicity: Toxicity may result in dizziness, fainting, slow heart rate, loss of bowel movement, and drowsiness. However, another incidence of a 36-year-old patient hat reported overuse of the injection with 66injections of 6mg taken within four weeks but with no adverse drug interactions observed physically or clinically.
Brand names
Imitrex, Embrace, Onzetra, Tosymra, Sumavel, and Treximet.
Generic name
Sumatriptan succinate
Dosing
Sumatriptan is available as a tablet indicated for migraines only, injection for migraines or cluster headaches, and a nasal spray for migraines or cluster headaches.
Tablet is available in strengths of 25mg, 50mg, and 100mg. The injectable solution is available in 6mg or 0.5 vials. The prefilled syringe cartridge is available in 3mg/0.5 mg auto-injector, 4mg, and 5mg forms.
Patients take the tablet as a whole without crushing or chewing. Additionally, a patient should not exceed 100mg per dose. However, if the migraine improves and then comes back, a patient is allowed to take the same dose again after two hours. If the first dose does not help, a patient is advised not to take the same medication for the same attack. Ultimately, the recommended maximum dose should not exceed 300mg/day.
An injection is available as an auto-injector in the strength of 6mg. If the first dose does not provide relief, a patient can repeat it after an hour of the first dose but should not exceed the overall dose of 12mg a day.
cluster headache
patients are expected to inject prefilled syringe that contains 6mg Sumatriptan directly into the thigh. It takes effect within ten to fifteen minutes. If the headache reduces and then comes back, the patient is expected to wait after an hour and inject another. If the first injection did not help, the patient should not repeat the same medication for a similar attack. The doctor might titrate a lower dose under certain circumstances, like when the patient experiences adverse reactions.
Dosage may also be modified when there is mild to moderate hepatic impairment, and the oral route takes the brunt, with the dosage slashed to 50mg/dose.
Indications for use
Sumatriptan is indicated for the treatment of migraines and cluster headaches. It is also FDA-approved to relieve photophobia and functional disability.
Sumatriptan is contraindicated in patients with severe hepatic impairment. It is also contraindicated for adults over sixty-five years. Children below twelve years are also not allowed to take the medication unless a specialist doctor prescribes it. Individuals with a history of coronary heart disease, angina, abnormal heart rhythm, and heart attack are also advised against it. Individuals with hypertension, peripheral heart disease, stroke, or seizures should also inform the doctor prior to prescription.
Additionally, pregnant patients who are trying to get pregnant or lactating patients should tell their doctor beforehand. Patients with known drug allergies should also inform the doctor before the prescription. The pharmacist or doctor should give an okay for those with latex allergies before administering the drug. St. Johns Wort is also contraindicated. After all, it risks increasing serotonin syndrome because it increases serotonin levels.
Pregnancy class
Animal studies have revealed several effects associated with lethality to the embryo, loss of fetal weight, increased pup mortality, decreased bone formation, and abnormalities of the skeletal tissue, with lethality to the embryo the most reported for doses that resulted in toxicity to the mother (Drugs.com, 2021). However, their results were only done on animal models, and there were no human pregnancy samples to serve as controls. The only data collected post-marketing on a thousand pregnant women was during the first trimester alone, and there were no patients that took it during the second or third trimester. The results were inconclusive, but there were no reports of fetal abnormalities.
In AU, TGA classifies Sumatriptan as pregnancy category B3 for drugs that have been taken by a limited number of women of childbearing age without evidence of harm to the fetus observed in animal samples (Drugs.com, 2021). The FDA classifies Sumatriptan as pregnancy category C for drugs that showed potential risks in animal studies in the US. However, the benefits far outweigh the potential risks associated with taking it. For these reasons, Sumatriptan is only given to pregnant women when the benefits outweigh the risks.
Breastfeeding warnings are that subcutaneous Sumatriptan injection is excreted into breast milk but has poor oral bioavailability, and thus amounts ingested by infants are small. However, the effects on infants are unknown (Drugs.com, 2021). Patients are thus encouraged to minimize infant exposure by breastfeeding eight to twelve hours after treatment with Sumatriptan.
Migraines have become one of the troublesome social diseases affecting close to 12% of the total world population. It is more common in individuals aged between thirty-five and forty years. Triptans are the best choice drugs for the treatment of migraines despite their higher cost and short relief times. Research conducted on the cost-effectiveness of selective 5HT1 receptor agonists in Ukraine found that the economic burden was on the consumer because the medication was effective yet short-lived.
Packaging with the same dose of the active ingredient with more tablets in the blister was more cost-effective compared to importing the same medication. (Hrynkiv et al., 2021) Additionally, it was more economical to use the 50mg packaging six tablets a blister during the dosage of Sumatriptan compared to any other doses. Value for a single tablet was calculated by finding the quotient of the cost of a single pack divided by the number of tablets. Using the quotients for all the brand names and dividing by the total number of brand names calculated the average cost for all the tablets.
According to the online drug database, the Imitrex syringe kit of 4mg and 6mg goes for 229.02 USD each, and the refill is roughly 216.92USD. Sumatriptan kit 6mg goes for 191.84USD and a refill of 4mg and 4mg for 184.46USD each (“Sumatriptan,” 2022). Imitrex 6mg vial goes for 106.84, and Imitrex 6mg solutions vial for 98.93USD. Imitrex nasal spray and inhaler range from 55.49USD- to 43.44USD. On average Imitrex 25mg, 50mg, and 100mg tablets go for 32.45, 30.16, and 30.16USD respectively. Sumatriptan 25mg, 50mg, and 100mg tablets go for 27.06, 26.15, and 26.15USD respectively. These figures depict Sumatriptan as superior in adherence to patients yet cheaper than its brand names.
Case study on patients under Sumatriptan
In a clinical trial where a placebo was used as a control, Sumatriptan administered orally, subcutaneously, and intranasally had better efficacy results than placebo in relieving migraine headaches and resolving symptoms associated with migraines like migraines dizziness, nausea, and pain (Lin et al., 2020). Additionally, the results also showed an improvement in clinical disability compared to placebo. Despite pain recurring in most care after the first dose, the second dose resolved the migraines.
Comparatively, subcutaneous Sumatriptan was shown to be more effective in resolving migraines compared to other drugs used to control migraines. Additionally, subcutaneous Sumatriptan resolved migraines at a higher rate than other forms of Sumatriptan administration, oral and nasal. Treatment of migraines using subcutaneous Sumatriptan resulted in less loss of work days compared to other treatment methods. Subcutaneous Sumatriptan resulted in resolution rates of migraines similar to other triptans. Patients also reported a higher quality of life when treated with Sumatriptan compared to those that received a placebo or other triptans.
Safety and efficacy results of Sumatriptan show that patients under Sumatriptan had better safety and efficacy results compared to placebo (Lin et al., 2020). Additionally, tolerance was higher in the patients as they experienced the common side effects associated with the oral drug of nausea, vomiting, fatigue, and malaise. Adverse reactions experienced by most patients with subcutaneous injection included injection site reactions. Nasal administration was associated with a bitter taste in the back of the mouth and irritation. Very few patients experienced adverse reactions because all contraindicated patients were excluded from the study.
In another case study, a combination of Sumatriptan and naproxen was used to treat migraines with or without auras in patients twelve years and older, and it was very successful (Greb, 2021). The combination was synergistic because a nonsteroidal anti-inflammatory drug combined with a triptan addresses pain, and the other reduces inflammation. The studies showed similar results compared to Sumatriptan alone, only that they were more efficacious. The benefits were sustained, and fewer patients had to go for a second dose. The combination was also linked to a significant reduction in physical disability compared to placebo.
Additionally, patients experienced more freedom from pain compared to single-dose triptans or a nonsteroidal anti-inflammatory drug alone. Additionally, the progression of symptom reduction was linear, with patients experiencing change within two hours to a whole day. Adverse effects experienced also reduced compared to placebo as fewer patients experienced dizziness, paresthesia, and somnolence. The group did not have adverse reactions because all contraindicated patients were excluded from the study.
Appropriate patient education centers on the indications for use and what patients should look for when taking the medication (NHS, 2019). A patient should not take more than 300mg/day of the oral dose, 12mg/day of injection, and 40mg/day of nasal spray. An overdose may result in drowsiness, dizziness, loss of control of bowel movement, slowed heart rate, and vomiting. The mode of action is to reduce vasodilation, which may result in constricted blood vessels leading to problems like abnormal heart rhythm and chest pains. In case of an overdose, a patient should have someone take them to the hospital in addition to carrying the packet of drugs together with all remaining medication the patient could have been taking.
Sumatriptan is not suitable for some people, and patients should tell the doctor all the relevant information before the prescription. They should disclose if they have had an allergic reaction to Sumatriptan or any other medication in the past (NHS, 2019). They should also disclose if they have a heart problem, like angina or abnormal rhythm. They should also disclose if they have previously had circulation problems or swelling in the extremities. They should also disclose if they have a history of stroke or any ischemic attacks. They should also disclose if they have hepatic problems. Patients should also tell their doctor if they have high blood pressure or suffer from seizures or fits. Patients should also disclose if they are heavy smokers or are on nicotine replacement therapy.
Several side effects are associated with taking Sumatriptan, most of them manageable through home remedies. Managing nausea would include eating small portions of meals, eating blunt foods, voiding dehydration by taking frequent sips of water, and maintaining rest. A patient can manage to feel dizzy by resting or lying down to avoid the chances of falling. If a patient feels a hot flush, they should be patient, and it will go away. However, they should contact their doctor after a prolonged period if they do not. Irritation by the nasal spray only lasts a short time and would thus not pose any future trouble. Patients can resolve bad taste in the mouth by chewing gum. If they have inflammation on injection sites, it will go away after a few days, but they should contact the doctor if it causes more irritation or inflammation.
Human data, though insufficient, indicates that Sumatriptan is not contraindicated in pregnancy. However, animal trial data suggests the medication causes several fetal complications (NHS, 2019). The drug is classified as category C by the FDA. Breastfeeding mothers on Sumatriptan have little to worry about. Small amounts of Sumatriptan pass through breast milk, and the amount that does is probably poorly metabolized because oral Sumatriptan is poorly metabolized and absorbed. Patients need to disclose to the doctor if they are pregnant, breastfeeding, or trying to get pregnant.
Several medications interfere with the mechanism of action of Sumatriptan. Patients should thus tell their doctor if they are taking other migraine medication, are on antidepressants, or are on monoamine oxidase inhibitor drugs (NHS, 2019). Patients should avoid taking Sumatriptan with St John’s Wort because it increases the risk of serotonin syndrome. Patients are advised to take the medication as soon as the pain starts, not at the warning stage when the pain is about to start. Patients are also advised to swallow the medication and avoid chewing. Patients are also encouraged to read the instructions for each medication to familiarize themselves with any additional information relevant to their conditions.
Role of a nurse practitioner in prescribing Sumatriptan
Nurse practitioners have a mandate to prescribe medications in all states, including narcotics, antibiotics, and many more. However, narcotics are divided into schedule II-V based on their effect on the body hence the restrictions on prescription in several states. Sumatriptan falls into a drug group called triptans that nurse practitioners can prescribe (“APRN’s role in ethical prescribing | Duquesne University,” 2020). A nurse should assess for side effects associated with administering injections like burning, numbness, itching, and feeling of pressure. A nurse should also assess the stress levels and any mechanism of coping with migraines. The nurse should also assess behavioral characteristics that predispose patients to migraines like caffeine intake, poor sleep, taking little water, or stress and issue advisory remarks. A nurse practitioner should thus evaluate and define the patient’s problem to ensure there is no other root cause.
A nurse practitioner should determine the therapeutic objective of the drug therapy to prescribe the correct medication (“APRN’s role in ethical prescribing | Duquesne University,” 2020). A nurse practitioner should also provide the patient with the relevant warnings and instructions regarding the medication. A nurse practitioner should also regularly monitor the patient to make appropriate dosage decisions. The practitioner should also consider the cost of medication, and use an appropriate tool to prescribe to avoid medication errors.
Monitoring and follow-up
The elimination half-life is one to four hours. Sumatriptan reaches maximum therapeutic concentrations ranging from 69.5 ng/ml to 12.9ng/ml. The daily dose for adults should not exceed 300mg for oral administration, 40mg for intranasal sprays, and 12mg for subcutaneous injections. The medication is contraindicated with St. Johns Wort, benzodiazepines, paroxetine, acetaminophen, fluoxetine, and duloxetine.
APRN’s role in ethical prescribing | Duquesne University. (2020, May 20). Duquesne University School of Nursing. https://onlinenursing.duq.edu/blog/aprns-role-responsibility-ethical-prescribing/
Drugs.com. (2021, August 12). Sumatriptan pregnancy and breastfeeding Warnings. https://www.drugs.com/pregnancy/sumatriptan.html
Greb, E. (2021, June 22). Novel NSAID–triptan drug effectively relieves migraine pain. Medscape. https://www.medscape.com/viewarticle/953519#vp_2
Hrynkiv, Y., Zaliska, O., Maksymovych, N., & Blavatska, O. (2021). Cost analysis of migraine pharmacotherapy with selective 5HT1 receptor agonists in Ukraine. Pharmacia, 68(1), 235-241. https://doi.org/10.3897/pharmacia.68.e51740
Lin, B., Zhou, Z., & Venkatesan, T. (2020). Sumatriptan as abortive treatment in cyclic vomiting syndrome: A cross-sectional study. Cephalalgia Reports, 3, 251581632095817. https://doi.org/10.1177/2515816320958174
NHS. (2019, October 21). Sumatriptan: A medicine to treat migraines and cluster headaches. nhs.uk. https://www.nhs.uk/medicines/sumatriptan/
Sumatriptan. (2022, May 5). DrugBank Online | Database for Drug and Drug Target Info. https://go.drugbank.com/drugs/DB00669

Drug Pharmacology and Pharmacokinetics

Our Service Charter

1. Professional & Expert Writers: Nursing Solved only hires the best. Our writers are specially selected and recruited, after which they undergo further training to perfect their skills for specialization purposes. Moreover, our writers are holders of masters and Ph.D. degrees. They have impressive academic records, besides being native English speakers.

2. Top Quality Papers: Our customers are always guaranteed of papers that exceed their expectations. All our writers have +5 years of experience. This implies that all papers are written by individuals who are experts in their fields. In addition, the quality team reviews all the papers before sending them to the customers.

3. Plagiarism-Free Papers: All papers provided by Nursing Solved are written from scratch. Appropriate referencing and citation of key information are followed. Plagiarism checkers are used by the Quality assurance team and our editors just to double-check that there are no instances of plagiarism.

4. Timely Delivery: Time wasted is equivalent to a failed dedication and commitment. Nursing Solved is known for timely delivery of any pending customer orders. Customers are well informed of the progress of their papers to ensure they keep track of what the writer is providing before the final draft is sent for grading.

5. Affordable Prices: Our prices are fairly structured to fit in all groups. Any customer willing to place their assignments with us can do so at very affordable prices. In addition, our customers enjoy regular discounts and bonuses.

6. 24/7 Customer Support: At Nursing Solved we have put in place a team of experts who answer to all customer inquiries promptly. The best part is the ever-availability of the team. Customers can make inquiries anytime.