|Year : 2018 | Volume
| Issue : 1 | Page : 26-29
Drug Dialogues – Medication news and new medications
|Date of Web Publication||27-Apr-2018|
Source of Support: None, Conflict of Interest: None
|How to cite this article:|
. Drug Dialogues – Medication news and new medications. Curr Med Issues 2018;16:26-9
Source: CMC Pharmacy Bulletin, a publication of the Pharmacy Service (DISH), CMC, Vellore.
Magic mushrooms to mitigate low mood
Psilocybin, a psycho- active component of Magic mushrooms, is thought to have therapeutic potential in psychiatric disorders but its mechanism of action within the brain is unclear.
In a study, researchers gave two doses of psilocybin to 19 patients with treatment resistant depression, and studied blood flow within the brain using functional magnetic resonance imaging (MRI) at baseline and one day after the last dose.
The The team found that depressive symptoms were significantly reduced in all patients at one week, and 47% showed a response at five weeks. There were decreases in blood flow to the temporal cortex, including the amygdala, and area associated with emotion processing, which correlated with the reduction in depressive symptoms.
Writing in Scientific Reports (13 Oct, 2017), the researchers said the findings were the first time that psilocybin had been shown to change brain activity outside of the active treatment period.
Carhart-Harris R, Roseman L, Bolstridge M et al. Psilocybin for treatment-resistant depression: fMRI-measured brain mechanisms. Sci Rep 2017;7:13187.
Angiotensin II approved to treat hypo-tension
The US Food and Drug Administration (FDA) has approved angiotensin II injection for intra-venous infusion to increase blood pressure in adults with septic shock.
In a clinical trial of 321 patients with shock and a critically low blood pressure, significantly more patients responded to treatment with angiotensin II compared to those treated with placebo. Angiotensin II effectively increased blood pressure when added to conventional treatments used to raise blood pressure.
Angiotensin II can cause dangerous blood clots with serious consequences, prophylactic treatment for blood clots should be used.
Source: FDA News Release [online, 21 Dec 2017]
Device to treat dry-eye syndrome
An intranasal neuro-stimulator device has been shown to significantly increase tear production in a one-day crossover study of 48 patients with dry-eye.
In the research presented at the American Academy of Ophthalmology Annual Meeting (12 Nov, 2017), a team studied the efficacy of a neurostimulator device for increasing tear production in people with moderate-to-severe dry eye.
One-day crossover study with 48 patients, the team showed that applying the device intranasally resulted in significantly greater tear production (25.3 mm/min) com-pared with both a placebo device (9.2 mm/min) and applying the device extranasally (9.5 mm/min).
The researchers followed 97 patients who used the device over 180 days, finding significantly greater tear production following neurostimulation than previously (17.3 mm/min vs 7.9 mm/min).
No serious device related adverse events were reported.
The team said the results indicated that the neurostimulation technology increased acute and long-term tear production in dry-eye.
Holland E, Baba S, Senchyna M et al. Intranasal tear neurostimulation for subjects with dry eye disease: results from 2 pivotal clinical trials. 121st Annual Meeting of the American Academy of Ophthalmology, New Orleans, Louisiana, 11–14 November 2017
Possible first drug to hunt down Huntington
The first human trial of a drug for Huntington’s disease has shown it to be safe, well-tolerated and successful in lowering the level of huntington protein in the nervous system.
The phase I/IIa trial comprised 46 patients with early Huntington’s disease at nine study centres in the UK, Germany and Canada. Each patient received four doses of either the drug, IONIS-HTTRx, or placebo. As the trial progressed, the dose of the drug was increased several times.
The results showed for the first time that IONIS-HTTRx, which is given by injection into the spinal fluid to enable it to reach the brain, significantly lowered the level of the toxic mutant hunting-ton protein, the protein known to cause the Huntington’s disease.
For the first time, a drug has lowered the level of the toxic disease-causing protein in the nervous system, and the drug was safe and well-tolerated.
The Pharmaceutical Journal, PJ December 2017 online.
Pharmacotherapy Lessons – Androgenetic alopecia
Male androgenetic alopecia (also known as androgenic alopecia or male pattern hair loss and male balding) is a common, progressive form of hair loss distinguished by the reduction of terminal hairs on the scalp in a characteristic distribution.
Although androgenetic alopecia is a benign and asymptomatic disorder, cosmetic concerns lead some patients to seek treatment.
The primary pharmacologic therapies for men with androgenetic alopecia are topical minoxidil and oral finasteride. Hair restoration surgery can also result in cosmetic improvement.
- Topical minoxidil and oral finasteride are the drugs that have been most extensively studied for the treatment of androgenetic alopecia.
- The response to treatment with finasteride or minoxidil varies.
- Some men achieve significant hair re-growth, while some others benefit from the slowing of additional hair loss.
- Continuation of these drugs is required to maintain results of therapy.
- Oral inhibitor of dihydrotestosterone (DHT) production
- Competitively inhibits the 5-alpha reductase type 2 enzyme, and thereby inhibits
- conversion of testosterone to DHT
- At a dose of 1 mg/day, the drug lowers serum and scalp DHT levels by more than 60%
- The drug has no affinity for androgen receptor and does not interfere with testosterone action
- The recommended dose is 1 mg/day
- Treatment should continue for at least 12 months to assess the drug’s full effects
- Hair regrowth will be lost over six to nine months if the drug is discontinued
- Occasionally finasteride results in erectile dysfunction, decreased libido, and ejaculatory dysfunction
- Promotes hair growth by increasing the duration of anagen, shortening telogen, and enlarging miniaturized follicles
- Due to greater efficacy of 5% topical solution compared with 2% solution in men, use of 5% solution is recommended
- Minoxidil solution is to be used for an indefinite time
- Apply 1 mL of solution twice daily to involved areas on a dry scalp using finger
- Hair shedding may occur at the initiation of treatment which usually resolves with-in two months
- Minoxidil should be used for at least four months to evaluate the response
- Side-effects are infrequent and the common ones include contact dermatitis and irritant dermatitis
Donovan J, Goldstein BG, Goldstein AO. Treatment of androgenetic alopecia in men. UpToDate [online, 07, Feb 2017]
Serious heart problems and deaths with loperamide use
The US Food and Drug Administration (FDA) continues to receive reports of serious heart problems and deaths with much higher than the recommended doses of loperamide, primarily among people who are intentionally misusing or abusing the drug. Loperamide is otherwise a safe drug when used as directed.
Loperamide acts on opioid receptors in the gut to slow the movement in the intestines and decrease the number of bowel movements. It is safe at approved doses, but when much higher than recommended doses are taken, it can lead to serious problems, including QT interval prolongation, Torsades de Pointes or other ventricular arrhythmias, syncope and cardiac arrest. Healthcare professionals are recommended to counsel patients to take loperamide only as prescribed and advice patients that drug interactions with commonly used medicines may in-crease the risk of serious cardiac events. Patients taking loperamide should also be informed to seek medical attention if experiencing any of the following: fainting, irregular cardiac rhythm or unresponsiveness.
FDA is continuing to evaluate this safety issue and will update the public when more information is available.
Source: FDA News Release
Did you know you can completely avoid Red man syndrome with vancomycin?
Regardless of its adverse effects on kidney and blood, vancomycin is often perceived precious due to its anti-MRSA activity and cost-effectiveness. Vancomycin induced hypersensitivity reactions are common. The most common adverse reaction, the ‘red man syndrome’ (RMS) is a rate dependent infusion reaction, not a true allergic reaction. RMS occurs principally with parenteral administration of vancomycin and is characterized by flushing, erythema, and pruritus, usually affecting the upper body, neck, and face more than the lower body. Pains and muscle spasms in the back and chest, dyspnoea, and hypotension may also occur.
In one study, 10 patients received vancomycin 1 gram rapidly over 10 minutes for surgical prophylaxis. All developed RMS, seven had severe cutaneous reactions, and five had a reduction in blood pressure of 20% or more, necessitating discontinuation of the infusion.
Another study compared the incidence and severity of RMS following administration of 1 gram vancomycin over one or two hours in 10 adult male volunteers. Eight individuals developed RMS with the one-hour infusion compared with three (mild) with two-hour infusion.
To avoid RMS, it has been suggested that vancomycin should be infused at a rate no higher than 10 mg/min OR 1 gram dose over 100 minutes (whichever results in slower infusion).
1.Renz CL, Thurn J, Finn H, Lynch J, Moss J. Oral antihistamines reduce the side effects from rapid vancomycin infusion. Anesth Analg. 1998;87(3):681.
2.Healy D, Sahai J, Fuller S, Polk R. Vancomycin-induced histamine release and “red man syndrome”: comparison of 1- and 2-hour infusions. 1990;34(4):550.
Pharmacotherapy Lessons - Severe Cancer Pain
Pain is a complex symptom that affects most aspects of life including physical functioning, daily activity, psychological and emotional status, and social life. The International Association for the Study of Pain defines pain as “an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage.” Pain is one of the most common symptoms in cancer patients. Cancer pain can be either acute or chronic. Treatment options depend mainly on characterization of pain. A commonly used approach to pain management employs the World Health Organization (WHO) pain relief ladder, which is a three-step ladder: if pain occurs, there should be prompt oral administration of drugs in the following order: non-opioids (aspirin and paracetamol); then, as necessary, mild opioids (tramadol); then, strong opioids such as morphine, until the patient is pain free.
- For severe pain, strong opioids are routinely used; morphine is often considered the opioid of choice because of its familiarity, broad availability, and lower cost
- Management of acute pain begins with immediate-release (IR) morphine. After stabilization, cumulative morphine dose over the past 24 hours can be converted to twice daily (once daily product is not available in CMC) modified-release preparation (MR). Use of IR morphine can be continued for breakthrough pain
- In patients unable to swallow, subcutaneous morphine is as effective as the intravenous route.
- Buprenorphine is a partial opioid agonist available as transdermal patch (one patch per week) and injection
- The drug is commonly used for chronic pain and it has a ceiling effect for analgesia and may induce QT prolongation at high doses (>20 mcg/h)
- Buprenorphine may cause less constipation and nausea than do other opioids
- Fentanyl is a highly lipophilic opioid available as transdermal patch and injection
- Transdermal patch is used for chronic pain (replaced once every 3 days)
- Fentanyl may be preferred over morphine in patients with renal insufficiency due to lack of active metabolites
- Exposing fentanyl patch to heat (e.g. Elevated body temperature) may cause unintentional increase in systemic fentanyl absorption, which may increase the risk of respiratory depression
Tramadol and tapentadol:
- Tramadol and tapentadol are centrally acting drugs acting both as mu agonists and MAOIs
- Tramadol is used for moderate pain while tapentadol is used for severe pain
- Up to 400 mg/day of tramadol with or without paracetamol is used orally (IM/IV up to 600 mg/day); the maximum daily dose of tapentadol is 500mg
- Codeine and pethidine are pure mu agonists which are not preferred in cancer pain mainly due to their toxicity
- Pentazocine, a mixed agonist-antagonist opioid is also not preferred for cancer pain due to its ceiling effect for analgesia
1. Cancer pain-Health professional version. NIH; Aug 2017
2. Cancer pain management with opioids: optimizing analgesia. UpToDate [Mar 2018]
Quantum Leaps in Medicine: Discovery of morphine
Last year, morphine celebrated its 200th anniversary as an analgesic ( first distributed for public use in 1817). Derived from the seedpods of the poppy, opium (Papaver somniferum) has been used since several thousands of years back. A 6000 year old Sumerian tablet speaks of it and it became famous to the point where Egyptian pharaohs had it placed in their tombs. By the 700s AD, opium use had spread to India, China and Arabia.
In early 19th century, the young uneducated curious boy Freidrich Wilhelm Adam Serturner (1783 - 1841) a pharmacist assistant watched frustrated physicians complaining about the unpredictability of opium to his boss, who could only ask his suppliers for better quality. Realizing that the problem would never be remedied until dosages could become standardized, Friedrich sought to isolate the active ingredient in opium, from which predictable and reliable doses could then be produced.
Working in the evenings on the pharmacist’s old equipment, Friedrich eventually isolated a yellow-white crystal after submerging it in ammoniated water. The substance isolated was identified as an alkaloid (the first ever alkaloid isolated from a plant source) with the then available knowledge.
After conducting animal experiments and adjusting the dosages, Friedrich named his new drug for the Greek god of dreams, Morpheus, but to keep it consistent with standard drug naming policy, it was named as morphine.
However Friedrich’s discovery was not welcomed by medical community due to his lack of credentials and poor methodology. Discouraged Friedrich kept aside his discovery for years until he treated himself successfully with morphine when he developed toothache. Finding it safe, he tested his product among local children and confirmed the safety and efficacy subjectively. It was then his second round of experiment started with French physician Francois Magendie who published a paper on morphine’s analgesic and sedative properties in 1817 followed by companies marketing morphine for medical use.
After 200 years of successful use, morphine continues to stay at the top of WHO analgesic ladder for severe pain. Truly a quantum leap in the history of medicine.
1. The invention of morphine. www.todayifoundout.com [online accessed, 08 Mar 2018]
2. Even today, morphine remains a popular opioid analgesic. PJ [online, 16 Apr 2013]
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