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Kaopectate II
Medicine Brands

Kaopectate II: Mechanism of Action, Active Ingredient, Uses, and Side Effects

by Healthlinear
written by Healthlinear

Kaopectate II Active Ingredient

Kaopectate II contains Loperamide as an active ingredient. Loperamide is used to treat diarrhea.

Kaopectate II Mechanism of Action

Loperamide helps to minimize fecal incontinence and urgency by increasing the tone of the anal sphincter.

Kaopectate II Side Effects

  • Constipation
  • Fatigue
  • Blood in stool
  • Rash
  • Nausea
  • Vomiting
  • Abdominal pain
  • Difficulty in breathing

What is the difference between Kaopectate and Imodium?

Kaopectate contains bismuth subsalicylate as an active ingredient while Imodium has loperamide as an active ingredient. Both are used in the treatment of diarrhea and stomach upset.

How long does it take for Kaopectate II to work?

After taking a single dose of 4mg, Kaopectate shows the onset of anti-diarrheal action in an hour.

Kaopectate and Imodium are trade names of?

Loperamide; an anti-diarrheal drug, is sold under the following trade names:

  • Imodium
  • Kaopectate 1-D
  • Maalox Anti-Diarrheal
  • Pepto Diarrhea Control

Are Kaopectate and Imodium the same?

Kaopectate is a drug that is used to treat diarrhea, nausea, heartburn, indigestion, gas, and stomach distress. It works by assisting in the slowing down of microorganisms that can cause diarrhea.

Imodium Capsule is an anti-diarrhea medication. It should not be given to patients who have dysentery.

Can I take Imodium and Kaopectate at the same time?

Taking some medications at the same time can produce an interaction known as drug-drug interaction. Interactions can reduce the effectiveness of one or more of the medications involved. They can also make you more susceptible to negative effects of drugs.

As a result, you should avoid taking Imodium A-D and Pepto-Bismol / Kaopectate at the same time. Putting them simultaneously won't make them work better for you. Rather, it can put you at risk for untoward effects.

Before using Imodium A-D, Pepto-Bismol, or Kaopectate, consult your doctor if you are taking any other medications.

References

https://www.medicines.org.uk/emc/product/522#gref
Kaopectate 1-D (Generic Loperamide)
https://www.medicinenet.com/loperamide-oral_capsule_tablet/article.htm
https://www.webmd.com/drugs/2/drug-56331-4025/pepto-diarrhea-control-oral/loperamide-oral/details
https://www.medicoverhospitals.in/medicine/kaopectate
https://www.healthline.com/health/diarrhea/Imodium-ad-vs-pepto-bismol#interactions
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Miltefosine
CancerMedicines

Miltefosine: Uses, Contraindications, Side Effects, and Mechanism of Action

by Healthlinear
written by Healthlinear

Initially developed as an anti-cancer drug, Miltefosine is chemically a phosphorylcholine ester of hexadecanol. It is an anti-leishmanial drug. Miltefosine is the first medicine to be given orally as a membrane-active alkyl phospholipid to treat “Cutaneous and Visceral leishmaniasis”. It is an oral medicine that, unlike earlier traditional therapy such as pentavalent antimonial drugs, amphotericin B, and pentamidine, which are parenteral agents, increases the treatment base in the population and lowers healthcare expenses. Miltefosine is more effective than antifungal amphotericin B and other conventional therapies against resistant antimonial Leishmania isolates and has fewer adverse effects.

Miltefosine Mechanism of Action

The exact mechanism of action of the drug Miltefosine is unknown. However, the proposed mechanism of action of anti-leishmanial activity of the drug Miltefosine suggests that inside the infected-Leishmania cell the drug shows various effects via its detergent-like action disrupting intracellular membranes of the cell, ultimately resulting in a mechanism similar to apoptosis.

Miltefosine Pharmacokinetics

The drug is well absorbed following oral administration. The Bio-half-life of the drug is 150 to 200 hours after oral administration and clearance are 25-30 days. The drug shows minimal urinary excretion. Intact hepatocytes have a low choline release, with decreasing rates in the provided order:

Human>Rat>Dog

What is miltefosine used for?

  • Cutaneous leishmaniasis
  • Visceral leishmaniasis (more severe form, lethal if the disease is untreated)
  • HIV patients with visceral leishmaniasis

According to a study published in 2004, Leishmaniases were found in 88 countries, with a mortality of 12–14 million persons and 1.5–2 million new cases each year. The global death rate was around 60,000 persons per year among the 350 million people who live in endemic areas.

0.40.5 million cases of Visceral leishmaniasis occur in

  • India
  • Nepal
  • Bangladesh
  • Brazil
  • Sudan

1-1.5 million cases of Cutaneous leishmaniasis occur in

  • Afghanistan
  • Brazil
  • Iran
  • Sudan
  • Peru

Current stats show approximately 50,000 cases of Visceral leishmaniasis and around 1.5 M cases of Cutaneous Leishmaniasis occur annually with more than ninety percent cases of visceral leishmaniasis occurring in

  • India
  • Nepal
  • Bangladesh
  • Sudan
  • Ethiopia
  • Brazil

Out of all cases of cutaneous leishmaniasis, approximately 90% occur in

  • Brazil
  • Peru
  • Algeria
  • Saudi Arabia
  • Syria
  • Iraq
  • Iran
  • Afghanistan

Miltefosine Contraindications

1.      Pregnancy and Child-bearing age

Miltefosine is a toxin that causes birth defects (teratogenic). It should not be used during pregnancy. Because the medicine has a long half-life, contraception should be provided for at least two months if a woman of childbearing age is receiving treatment.

Is Meltifosine safe in pregnancy?

FDA assigns category D to this drug. Miltefosine should not be used if you are pregnant. Before beginning this medication, you may need to obtain a negative pregnancy test.

2.      Sjogren Larsson Syndrome

Patients with Sjogren Larsson Syndrome are unable to metabolize long-chain fatty alcohols like hexadecanol, and the buildup of this hexadecanol causes severe neurological abnormalities beginning in childhood. Because hexadecanol, long-chain fatty alcohol derived from Miltefosine disintegration, can be converted to palmitic acid and used in lipid biosynthesis or beta-oxidation, the therapy is not recommended for people who have a genetic abnormality connected to the rare Sjogren Larsson syndrome.

Miltefosine Side effects

  • Gastrointestinal toxicity (Mild to Moderate)
  • Nausea
  • Elevated levels of serum creatinine
  • Vomiting
  • Elevated serum aspartate aminotransferase
  • Elevated serum alanine aminotransferase
Nausea

Is Miltefosine Available in India?

India accounts for more than half of the world's kala-azar burden. In 2005, Miltefosine was commonly available without a prescription or a limit on the amount dispensed over the counter (OTC). When the medicine was marketed in private pharmacies in India, the possibility for resistance became a serious worry, and patients were compelled to accept shorter courses due to financial constraints. As a result, from 2008 forward, India only provided miltefosine to the public sector. Miltefosine's effectiveness is said to have dropped after being taken as monotherapy for over a decade.

Miltefosine Brand names

  • Miltex
  • Impavido
  • Miteforan

References

https://doi.org/10.1016/B978-008055232-3.63996-0
https://pubmed.ncbi.nlm.nih.gov/15225981/
https://doi.org/10.1016/B978-0-7020-6285-8.00123-4
https://www.scielosp.org/article/bwho/2005.v83n5/394-395/
https://gh.bmj.com/content/3/3/e000709
https://www.medindia.net/doctors/drug_information/miltefosine.htm
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Hydroxychloroquine
Medicines

Hydroxychloroquine: Uses, Mechanism of Action and Contraindications

by Healthlinear
written by Healthlinear

What is Hydroxychloroquine?

Hydroxychloroquine is a blood schizonticidal drug. It is classified as anti-malarial medication and is used in the treatment of malaria, rheumatoid arthritis, and systemic lupus erythematosus (SLE). It is also classified as a disease-modifying anti-rheumatic drug (DMARD). Hydroxychloroquine is also prescribed to prevent malaria in travelers to those countries where malaria is endemic. In the case of malaria treatment, the drug is only effective when malaria is uncomplicated.

Mechanism of Action of Hydroxyquinoline

Chloroquine and hydroxychloroquine raise the pH of intracellular vacuoles, affecting activities such as protein degradation by acidic hydrolases in the lysosome, protein post-translation modification in the Golgi apparatus, macromolecule assembly in endosomes. It binds to heme (preventing its polymerization to hemozoin which is non-toxic for the parasite) and increases the pH which eventually results in oxidative damage to the membranes.

This process leads to the death of the parasite as well as RBCs. When it comes to the drug’s anti-malarial activity, these two particulars i.e. binding of the drug to heme and prevention of its polymerization into parasite-friendly substance (hemozoin) have a central role.

The secretion of cytokines such as interleukin-1 and tumor necrosis factor is also reduced by hydroxychloroquine. It's suggested that the anti-rheumatic properties of the drug hydroxychloroquine and chloroquine are attributed to interference with "antigen processing" in antigen-presenting cells and macrophages.

Pharmacokinetics of Hydroxychloroquine

It shows 67-74% bioavailability. It shows plasma protein binding up to 50%. CYP3A4 N-dealkylates hydroxychloroquine to produce the active metabolite desethylhydroxychloroquine and the inactive metabolites desethylchloroquine and bidesethylchloroquine. The drug is eliminated from the body through urine, feces, and skin.

How to take Hydroxychloroquine?

It is advised to be taken with food or milk.

Who should not take Hydroxychloroquine?

Patients suffering from psoriasis should avoid taking hydroxychloroquine.

Who can take Hydroxychloroquine?

  • Children of all ages
  • Adults
  • Pregnant women

Is it safe in pregnancy?

The use of hydroxychloroquine is generally considered safe during pregnancy. If you're thinking about starting a family or if you become pregnant while taking it, talk to your doctor as soon as possible.

Can lactating mothers take hydroxychloroquine?

If you're using Hydroxychloroquine, you can still breastfeed. Even though the drug may enter into breast milk, it is unlikely to have any effect on the baby. The advantages of continuing to take it when you're pregnant or breastfeeding, the advantages usually exceed the risks.

Lactation

Where to Buy?

Antimalarial medications are only available by prescription in the United States. Medicines should be purchased before traveling rather than in the target country. Purchasing pharmaceuticals from a foreign country carries risks: the drugs may be of poor quality, contaminated, or counterfeit, and may not protect the individual from malaria.

Hydroxychloroquine Side Effects

Common side effects associated with the use of hydroxychloroquine include

  • Nausea
  • Abdominal pain
  • Headache
  • Dizziness
  • Nervousness
  • Sensory-motor disorders
  • Pigmentation
  • Urticarial
  • Hypoglycemia
  • Anemia
  • Bone marrow depression
  • Diarrhea
  • Vomiting
  • Retinal toxicity

In case of ocular effects, the drug should be immediately discontinued.

Hydroxychloroquine Drug Interactions

It shows interaction with the following drugs:

  • Amiodarone
  • Digoxin
  • Moxifloxacin
  • Antacids
  • Ciclosporin
  • Tamoxifen
  • Antidiabetic drugs
  • Acebutolol
  • Acetaminophen
  • Acetazolamide

How to take Hydroxychloroquine?

The drug is typically given twice a day. Each pill contains 200 milligrams. The normal dosage is one or two pills per day. This medicine should be used on a daily basis at the same time. It will take one to two months to get up and running. Follow your doctor's advice. Take only the amount of medicine prescribed. It's best to take this drug with food or milk. It is critical that your doctors know if you are taking any other medications while taking Hydroxychloroquine. Prescription and over-the-counter medications, as well as birth control pills, vitamins, and herbal supplements are all included.

Can I take it for covid prevention?

According to WHO, data of clinical trials upon prevention of Covid-19 by hydroxychloroquine suggests that the drug has little or no effect on illness or death.

Hydroxychloroquine Henry Ford study

Henry Ford's COVID-19 hydroxychloroquine trial was secretly stopped off after a while. In spring 2020, when erstwhile US President Trump pitched it as a potential game-changer, in the prevention and treatment of the then newly emerged coronavirus, it sparked some interest. However, early excitement gave way to larger medical research, with the country's top health agencies eventually concluding that it was ineffective in treating or stopping the spread of the new coronavirus. The trials were ended before Christmas 2020. Henry Ford announced the termination of the hydroxychloroquine project by stating that from now on, vaccines will be their primary objective of protecting their frontline healthcare workers.

How to take Hydroxychloroquine sulfate?

Take this drug by mouth as advised by your doctor, typically with food to avoid stomach problems. The dosage and duration of medication are determined by your medical condition and treatment response. Dosage is individualized as per body weight in children.

Can you take it with milk?

Yes. Hydroxychloroquine can be taken with milk or food.

Can it cause liver demage?

Metabolized in the liver, hydroxychloroquine can affect the way other drugs are processed. Therapy is unlikely to induce liver damage in healthy people, but it can cause an abrupt aggravation of porphyria cutanea tarda in a vulnerable population.

Hydroxychloroquine Indication

It is used to treat the following conditions:

  • Erythrocytic Plasmodium falciparum malaria
  • Plasmodium vivax malaria
  • Systemic lupus erythematosus (SLE)
  • Acute rheumatoid arthritis
  • Chronic discoid lupus erythematosus
  • Chronic rheumatoid arthritis
  • Porphyria cutanea tarda

Who makes it?

Name of some of the major manufacturers of hydroxychloroquine are

  • Sanofi
  • Pfizer
  • Novartis

Popular Brands of Hydroxychloroquine

  • Plaquenil

References

https://medlineplus.gov/druginfo/meds/a601240.html
https://go.drugbank.com/drugs/DB01611

Click to access hydroxychloroquine.pdf

https://clinicaltrials.gov/ct2/show/NCT02379650

Click to access hydroxychloroquine-leaflet-2014b.pdf

https://pubmed.ncbi.nlm.nih.gov/8278823/
https://www.cambridgeshireandpeterboroughccg.nhs.uk/easysiteweb/getresource.axd?assetid=11910&type=0&servicetype=1
Hydroxychloroquine (Plaquenil®) Drug Information Sheet
https://www.who.int/emergencies/diseases/novel-coronavirus-2019/advice-for-public/myth-busters?gclid=Cj0KCQjwxJqHBhC4ARIsAChq4auIsLWTkgWGZVp2W0fcRwRW776gQgjJn9TvRgNxpfcfqTYv_JqujPEaAtDwEALw_wcB#chloroquine
https://www.webmd.com/drugs/2/drug-5482/hydroxychloroquine-oral/details

Lippincott’s illustrated reviews Pharmacology 4th edition

https://www.freep.com/story/news/health/2021/01/11/henry-ford-study-hydroxychloroquine-covid-19/6625541002/
https://www.henryford.com/news/2020/08/hydroxychloroquine-an-open-letter
https://www.bridgemi.com/michigan-health-watch/henry-ford-study-hydroxychloroquine-covid-quietly-shut-down
https://www.medicines.org.uk/emc/product/11732/smpc/print#gref
https://www.ncbi.nlm.nih.gov/books/NBK548738/
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Auvi-Q
Medicine Brands

Auvi-Q (Epinephrine Injection): Uses, Dosage and Side Effects

by Healthlinear
written by Healthlinear

Auvi-Q contains epinephrine. It is a prescription medicine. It is used to treat anaphylactic shacks.

Auvi-Q Uses

This medicine is intended to treat severe allergic responses to insect stings/bites, foods, medications, or other substances in the event of an emergency. Epinephrine improves breathing, stimulates the heart, reverses hives, raises blood pressure, and reduces swelling in the face, lips, and neck promptly.

Side Effects of Auvi-Q

The most common side effects of Auvi-Q include:

  • Headache
  • Palpitations
  • Nausea
  • Vomiting
  • Dizziness
  • Nervousness
  • Anxiety
  • Sweating
  • Weakness
  • Breathing issues

The elderly population is at greater risk to experience adverse effects.

How to Use Auvi-Q?

  • It is a one-use injector.
  • Should only be injected into the area of the outer thigh.
  • Should not be injected in areas of fingertips, buttock, veins, hands, feet, and toes.

Degradation

Epinephrine is a light-sensitive drug. It should be protected from exposure to light. When exposed to air or light, epinephrine solution quickly degrades, turning brown from the creation of melanin, and pink from oxidation to adrenochrome. Patients should be instructed to visually inspect the epinephrine solution through the viewing glass regularly.

References

https://www.rxlist.com/auvi-q-drug.htm
https://www.auvi-q.com/
https://www.webmd.com/drugs/2/drug-163215/auvi-q-injection/details

Click to access 201739s008s009lbl.pdf

https://www.drugs.com/auvi-q.html

Image From: auvi-q.com

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Epinephrine
Medicines

Epinephrine (Adrenalin): Uses, Side Effects, Dosage, and Mechanism of Action

by Healthlinear
written by Healthlinear

What is Epinephrine?

Epinephrine, also known as adrenaline, is produced by the medulla of the adrenal glands. It is released into the bloodstream in response to strong emotions like fear or anger, causing increased heart rate, blood pressure, muscle strength, and sugar metabolism. Epinephrine has been classified as a sympathomimetic (Adrenergic agonist) catecholamine that uses a G protein-linked second messenger pathway to exert its pharmacologic effects on both alpha-adreno-receptors and beta-adrenoceptors.

What are the main functions of Epinephrine / Adrenaline?

Produced from tyrosine in the medulla of adrenal glands, epinephrine is released with small quantities of norepinephrine into the blood circulation. It causes vasodilation at low doses and at high doses it causes vasoconstriction. The "Flight or Fight Response," as it is known, prepares the body for vigorous activity. Epinephrine is a stimulant in cardiac arrest, a vasoconstrictor in case of shock, and a bronchodilator and an antispasmodic drug in bronchial asthma.

Mechanism of Action / What does epinephrine do?

In small quantities, it shows a great affinity for beta-adrenoceptors. In large doses, it shows selective affinity towards alpha receptors.

Alpha-1 effects

  • Increase in vascular smooth muscle contraction
  • Contraction of pupillary dilator muscles
  • Contraction of intestinal sphincter muscles

Beta-1 and Beta-2 effects

  • Contraction of the myocardium (beta-1 action, positive inotropic effect)
  • Increase in heart rate
  • Increased renin release
  • Bronchodilation (beta-2 action)
  • Vasodilation (beta-2 action)
  • Production of aqueous humor

Pharmacokinetics of Adrenaline / Epinephrine

How to administer it into the body?

It degrades rapidly, so it has a small duration of action, and the onset of its action is very rapid. To attain the most rapid onset, during emergencies, adrenaline is given via the IV (intravenous) route. Other routes of administration of epinephrine involve the subcutaneous route, intramuscular route, inhalational route, by endotracheal tube, neonatal resuscitation, and topically in the eye.

Can Adrenaline / Epinephrine be given orally?

It is not given orally because its oral administration is ineffective. Intestinal enzymes degrade the drug following an oral administration thus making it useless.

Metabolism

Just like other catecholamines, the metabolism of epinephrine involves two enzymatic pathways:

  1. Monoamine oxidase (MAO)
  2. Catechol-O-Methyl transferase (COMT)

How does it excrete out of the body?

Metabolites of epinephrine are excreted out of the body by urine.

Adrenaline / Epinephrine Uses

Following are the indications for use of epinephrine

  • Anaphylaxis
  • Cardiac arrest (used to bring back cardiac rhythm)
  • To treat open-angle glaucoma (used topically in the form of 2% epinephrine eye drops)
  • Local anesthetic
  • Acute asthma
  • Emergency treatment of type 1 hypersensitivity reactions
  • Hypotension because of septic shock
  • To induce and maintain mydriasis during ocular surgery

Use of Epinephrine in Pregnancy / Is it safe during Pregnancy?

Epinephrine can be used during pregnancy only if the possible benefit outweighs the danger to the fetus. It lies in pregnancy category C drugs. It crosses the placenta. No well-controlled human studies are available for the use of epinephrine. Animal studies have shown some teratogenic effects. Its use in pregnancy requires caution if the patient has high blood pressure i.e. 130/80mmHg or more.

According to American Dental Association, for diagnostic, preventive, and dental treatments, local anesthetics which are available in combination with epinephrine such as Bupivacaine, Lidocaine, and Mepivacaine can be used during pregnancy.

Adrenaline Contraindication

It is contraindicated in patients who have hypersensitivity to adrenergic agonists. Other contraindications of epinephrine may include:

  • Closed-angle glaucoma
  • Anesthesia with Halothane
  • Catecholamine polymorphic ventricular tachycardia
  • Peripheral arterial occlusive vascular disease with thrombosis
  • Ergot poisoning
  • Ventricular fibrillation

Toxicity

Epinephrine toxicity can be potentially lethal in some cases. The overall treatment of toxicity with adrenaline is primarily supportive. Many researchers have reported the use of Labetalol as an antidote to treat epinephrine overdose in certain cases.

Some specific conditions of epinephrine toxicity are given below

Increased beta-1 adrenergic effect

Treatment: Beta adreno-receptor blocking drugs such as Metoprolol

Presser effects

Treatment: Alpha adreno-receptor blocking drugs with respiratory support

Interactions with Other Drugs

Epinephrine shows interaction with the following drugs.

  • Cocaine and cyclic antidepressants
  • Monoamine oxidase inhibitors
  • Beta-blockers
  • Inhalational anesthetics
  • Digitalis
  • Halogenated general anesthetics and cyclopropane
  • Chloral hydrate
  • Catechol-O-Methyl transferase inhibitors
  • Diuretics
  • Anti-hypertensive drugs
  • Vasodilators

Epinephrine Side Effects

It produces the following side effects on various systems in the body:

  • Side effects related to the central nervous system include fear, tension, anxiety, Parkinson’s disease exacerbation, agitation, and tremors.
  • Because of an increase in blood pressure, the drug may cause a hemorrhage.
  • It may induce cardiac arrhythmias, tachycardia, palpitations, and chest pain.
  • The drug can trigger pulmonary edema.
  • Side effects related to the gastrointestinal tract include nausea and vomiting.
  • The drug may cause decreased renal perfusion
  • At the site of injection, epinephrine may result in necrosis on the skin.

Brand Name:

Auvi-Q brand name containing Epinephrine.

References

https://www1.udel.edu/chem/C465/senior/fall00/Performance1/epinephrine.htm.html

Lippincott’s illustrated reviews Pharmacology 4th edition

https://www.ncbi.nlm.nih.gov/books/NBK482160/
https://www.ada.org/en/member-center/oral-health-topics/pregnancy#:~:text=Preventive%2C%20diagnostic%2C%20and%20restorative%20dental,may%20be%20used%20during%20pregnancy.
https://www.drugs.com/pregnancy/epinephrine.html
https://pubmed.ncbi.nlm.nih.gov/2344087/
https://www.rxlist.com/adrenalin-drug.htm
https://accessmedicine.mhmedical.com/content.aspx?bookid=391§ionid=42070000
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Arsobal: Dosing, Uses, Contraindications and Side Effects
Medicine Brands

Arsobal: Dosing, Uses, Contraindications and Side Effects

by Healthlinear
written by Healthlinear

Arsobal contains Melarsoprol which is classified as an antimalarial drug. Melarsoprol is a drug that is used to cure African sleeping sickness, a parasitic infection.

Active Ingredient

Melarsoprol

Arsobal Side effects

Side effects of Arsobal include vomiting, hypertension, peripheral neuropathy, encephalopathy, and albuminuria.

Is it Safe in Pregnancy?

Arsobal is an investigational new drug (IND). There have been no studies conducted to determine the pregnancy category of this drug. In the US, it is not available commercially.

Arsobal Contraindications

  • Hypersensitivity
  • G6PD (Glucose-6-phosphate dehydrogenase) deficiency

Uses

Arosbal is used in the treatment of African sleeping sickness also known as African Trypanosomiasis.

Arsobal Dosage Form

It is available in parenteral dosage form. Contains 180 mg/5 mL (36 mg/mL) in a 5 mL glass ampule.

Who Manufactures Arsobal?

It is manufactured by Sanofi Aventis.

(Important* The drug is not commercially available in the US and Canada)

References

https://www.drugs.com/cons/arsobal.html
https://reference.medscape.com/drug/arsobal-melarsoprol-342662#0
https://www.cdc.gov/laboratory/drugservice/formulary.html
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Melarsoprol
Medicines

Melarsoprol: Doses, Indications, Uses and Side Effects

by Healthlinear
written by Healthlinear

In Africa, sleeping sickness has resurfaced. The few medications now approved to treat this disease, which is caused by parasite protozoa of the Trypanosoma brucei group, are being hampered by adverse side effects and treatment resistance. Before parasites emerge in the central nervous system, pentamidine and suramin are utilized. The major medicine used to treat late-stage sleeping sickness caused by Trypanosoma brucei subspecies is melaminophenyl arsenical Melarsoprol.

A trivalent organic arsenical Melarsoprol is used to treat trypanosomiasis (sleeping sickness). It is, however, a highly hazardous substance, and its usage has been abandoned in all stages of sleeping sickness except microencephalitic. Pentamidine and suramin, for example, are substituted.

Melarsoprol Mechanism of Action

Melarsoprol works by inhibiting energy production in the parasite. It binds irreversibly with the sulfhydryl groups on protein kinase. As a result, this enzyme is inactivated, and parasite glycolysis is disrupted. Many of the harmful effects of melarsoprol are due to sulfhydryl groups in other proteins reacting with arsenicals.

Melarsoprol Pharmacokinetics

Route of Administration

Melarsoprol is administered with a gradual intravenous (IV) injection. As the drug is extremely irritating to tissues, and additional precautions must be taken to avoid extravasation.

Melarsoprol Distribution

The medication concentration in the cerebrospinal fluid (CSF) is 2–20 percent of plasma levels, which is enough to produce trypanocidal effects.

Metabolism

Melarsoprol is quickly metabolized to various trypanocidal substances in the body (possibly melarsen oxide).

Elimination

Melarsoprol is quickly excreted from the body through the kidneys.

Melasoprol Side Effects

  • PTRE (Post-treatment reactive Encephalopathy) occurs in 5-10 percent of the patients treated with an above-mentioned drug, which may involve the following consequences
  • Mental deterioration
  • Headache
  • Tremors
  • Difficulty in speech
  • Coma
  • Convulsions
  • Death
  • Fever
  • Chest pain
  • Abdominal pain
  • Vasodilation
  • Disturbances of the smelling sense
  • Herxheimer-like reaction
  • Diarrhea
  • Jaundice
  • Conjunctival infections
Headache

Melarsoprol Contraindications

The drug is contraindicated in patients with

  • Known hypersensitivity
  • Severe hemolytic reactions (Glucose-6-phosphate dehydrogenase deficiency patients)
  • Renal impairment
  • Hepatic insufficiency
  • Hypertension
  • Arrhythmias
  • Myocardial ischemia
  • Heart failure
  • Epilepsy
  • Neuropathy
  • Leprosy

Melarsoprol Uses

The drug is used to treat African sleeping sickness also known as African Trypanosomiasis.

Why is Melarsoprol Toxic?

Melarsoprol works by binding with the sulfhydryl groups of protein and inactivating enzymes as a result of this nonspecific action. This mechanism is also responsible for the drug's toxicity. Melarsoprol is extremely dangerous. It irritates tissues, and extravasation must be avoided by using a fine gauge needle. Fever is a regular occurrence. Reactive encephalopathy usually develops within the first 3–4 days of treatment which affects up to 18% of patients and can be lethal.

What is Suramin?

Suramin is a drug classified as an anti-protozoal drug, that is used to treat T.b. gambiense and trypanosomiasis.

How Much Does Melarsoprol Cost?

A study conducted to estimate the cost-effectiveness of Eflornithine in comparison with Melarsoprol shows to treat the second stage of African Trypanosomiasis showed the following results:

  • Cost per patient $504.6
  • Cost per life saved $527.5

What is Trypanosomiasis Disease?

How someone gets infected with African sleeping sickness?

Micro-parasites of the species Trypanosoma brucei cause African Trypanosomiasis, commonly known as "sleeping sickness." The tsetse fly (Glossina species), which is only found in Sub-Saharan Africa, transmits the disease. In endemic countries, the tsetse flies that spread African trypanosomiasis can be found in rural areas.

African Trypanosomiasis disease course of progression

Sleeping sickness infection occurs in two phases: initially, the parasites are identified in the lymphatic system as well as in the blood, then the parasites infiltrate the central nervous system (CNS) in the second stage.

Sleeping sickness symptoms

Symptoms of sleeping sickness include severe headaches, irritability, intense weariness, fever, swollen lymph nodes, and painful muscles and joints. Some people get a rash on their skin. After the disease has infected the central nervous system, it causes progressive disorientation, personality changes, and other neurologic disorders (second stage). If the sickness is not addressed, it will worsen and eventually lead to death in a few months.

Consult your health care practitioner right away if you suspect you have African trypanosomiasis. Several tests may be used to detect the parasite such as,

  • Skin biopsy of the chancre
  • Blood tests
  • Spinal tap

For African trypanosomiasis, there is no curative test.

Melarsoprol Brand Names

Arsobal (It is not commercially available in the US)

References

https://pubmed.ncbi.nlm.nih.gov/11137702/
https://www.pediatriconcall.com/drugs/melarsoprol/182
https://journals.asm.org/doi/full/10.1128/AAC.48.9.3268-3271.2004
https://doi.org/10.1016/B978-008055232-3.62121-X
https://www.cell.com/trends/parasitology/fulltext/S1471-4922(18)30067-9

http://www.antimicrobe.org/drugpopup/Melarsoprol.htm

https://doi.org/10.1016/B978-0-7020-6285-8.00157-X
https://www.rxlist.com/consumer_suramin/drugs-condition.htm
https://pubmed.ncbi.nlm.nih.gov/18304274/
https://www.cdc.gov/parasites/sleepingsickness/gen_info/faqs.html
https://www.cdc.gov/parasites/sleepingsickness/treatment.html
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Ketamine
Medicines

Ketamine: Uses, Mechanism of Action, Side Effects, and Contraindications

by Healthlinear
written by Healthlinear

What is Ketamine and what does it feel like?

Non-barbiturate general anesthetic ketamine is a short-acting drug that is used to induce a kind of unconsciousness in patients where they feel no pain but appear to be awake. This state is called dissociated state and so does ketamine called dissociative anesthesia. Immobility, amnesia, and sedation are primary outcomes associated with the use of ketamine.

Calvin Stevens of Parke Davis Laboratories developed Ketamine in 1963 as a substitute for phencyclidine (PCP). It was first employed for veterinary purposes in Belgium, and it was observed in 1964 that it caused mild hallucinogenic effects and shorter psychotomimetic effects when compared to PCP.

It was licensed by the FDA in 1970 and has since been used as a local anesthetic for children and people having minor procedures and in animals. However, the drug is not used widely because it encourages postoperative hallucinations and an increase in cerebral blood flow.

Ketamine Mechanism of Action

By reacting with N-Methyl-D-aspartate (NDMA) receptors, the drug produces an analgesic effect. The aforementioned mechanism is also said to be involved in the neuroprotective mechanism of the drug. Ketamine stimulates central sympathetic flow, which stimulates the heart and increases blood pressure as well as cardiac output. Owing to this, the drug is a very suitable candidate for hypovolemic, asthmatic, and cardiogenic shock patients.

Ketamine Pharmacokinetics

Absorption

Ketamine is rapidly absorbed and has a bioavailability of roughly 93 percent. Only 17 percent of the prescribed dosage is absorbed after the first pass effect. It spreads quickly and has a distribution half-life of 1.95 minutes.

Plasma Protein Binding

53.3% of the administered dose is bound to plasma proteins.

Metabolism

The drug undergoes hepatic metabolism producing norketamine.

Mechanisms of biotransformation involved in the metabolism of ketamine may involve

  • N-dealkylation
  • Hydroxylation of the cyclohexane ring
  • Conjugation to glucuronic acid
  • Dehydration of the hydroxylated metabolites for the formation of cyclohexene derivatives

How Ketamine is Eliminated?

It is primarily eliminated from the body in urine. Some amounts of the drug are also excreted in bile and feces.

Ketamine Adverse Effects

Ketamine infusions at sub-anesthetic levels can cause a variety of side effects, most of which occur during the infusion phase and fade away quickly. Among the acute and transitory side effects are:

  • A rise in blood pressure
  • Perceptual disturbance
  • Drowsiness
  • Dizziness
  • Nausea
  • Vomiting
  • Dissociation
  • Floating sensation
  • Vivid pleasant dreams
  • Nightmares
  • Hallucinations
  • Delirium
Nausea

What is Ketamine Used for?

Historical uses associated with ketamine

For nearly 50 years, ketamine has been utilized in the operating room. In patients with asthma or life-threatening acute bronchial constriction, ketamine's bronchial dilating characteristic makes induction and maintenance of anesthesia safer.

The drug is also one of the few medications that can be used to induce anesthesia during a cesarean section. It is the preferred agent in the treatment of children and burns sufferers. Additionally, ketamine treatment during induction may reduce postoperative delirium, particularly in patients on cardiopulmonary bypass.

Ketamine Current Uses

Ketamine has appeared as a promising medicine for nearly half a century after its discovery to treat

  • Preoperative and postoperative pain
  • Depression
  • Inflammation

Ketamine Contraindications

The use of the drug is contraindicated under the following conditions:

  • Hypersensitivity
  • Aortic dissection
  • Uncontrolled hypertension
  • Myocardial infarction
  • Aneurysms
  • Obstetrics
  • Pregnancy
  • Breastfeeding
  • Chronic alcoholics
  • Patients with acute Alcohol intoxication
  • Schizophrenia
  • Elevated levels of Cerebrospinal fluid (CSF)
Lactation

Ketamine Abuse

Ketamine and its synthetic analogs have become drugs of abuse having hallucinogenic effects, in addition to its legitimate, medical usage.  It is frequently insufflated ("snorted") up the nose when abused in social contexts. It can also be injected, taken orally as a liquid, or smoked in the form of marijuana or tobacco. It's commonly taken in conjunction with other drugs like cocaine or amphetamines. Multiple drug use has resulted in death.

Long-term usage can lead to psychological dependence. When chronic users stop taking the drug, they will suffer cravings, making it difficult to quit because their bodies are not accustomed to operating without it.

Ketamine Therapy

Ketamine is injected into a vein (IV) or a muscle (IM). The FDA recently approved a ketamine nasal spray for the treatment of patients with treatment-resistant depression.

How Long does Ketamine Stay in your System?

Ketamine is a short-acting anesthetic drug. Ketamine's effects might last anywhere from 5 to 30 minutes, depending on how it's administered.

Infusion

Ketamine has been proved to have antidepressant qualities in studies for decades. The United States Food and Drug Administration (FDA) has licensed ketamine for the induction and maintenance of anesthesia, as well as the treatment of psychiatric illnesses and chronic pain. Ketamine has been used to treat psychiatric diseases such as MDD, bipolar disorder, and post-traumatic stress disorder (PTSD), and post-operative and chronic pain management.

For the treatment of psychiatric problems, ketamine infusion therapy comprises giving a single infusion or a series of infusions. For example

  • Major depressive disorder
  • Post-traumatic stress disorder
  • Acute suicidality

Ketamine Brand Names

Following are some brand names containing Ketamine:

References

https://pubmed.ncbi.nlm.nih.gov/9707750/

Lippincott Illustrated Reviews: Pharmacology 4th edition

https://go.drugbank.com/drugs/DB01221
https://journals.sagepub.com/doi/10.1177/2045125320916657
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4933765/
https://www.ncbi.nlm.nih.gov/books/NBK470357/
https://americanaddictioncenters.org/ketamine-abuse/how-long-does-ketamine-stay-in-your-system
https://www.apna.org/m/pages.cfm?pageid=6603
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Imodium
Medicine Brands

Imodium A-D Uses, Side effects and Interactions

by Healthlinear
written by Healthlinear

Loperamide is marketed under the brand name Imodium, which is also stylized as Imodium A-D. Imodium, unlike Lomotil, is available over-the-counter (OTC). As a result, it's more generally accessible.

How does Imodium work?

Imodium contains Loperamide HCl as an active ingredient. It works by decreasing peristaltic movements.

Imodium A-D Side Effects

  • Drowsiness
  • Dizziness
  • Dry mouth
  • Constipation
  • Flatulence
  • Nausea

How long does Imodium take to work?

The onset of action of Imodium is one hour. Once you orally take the medicine, it takes almost an hour when the drug shows its effect.

How long does Imodium last?

It takes roughly 11 hours for the level of Imodium in your body to drop by half after you stop taking it. Imodium will have less and less of an effect on regulating your diarrhea after this period of time. The medicine will usually be eliminated from your body in 2 to 3 days.

Imodium A-D Uses

diarrhea

Is it safe to take Imodium during pregnancy?

It may be safe to take Imodium as directed on occasion during pregnancy, but there is no evidence that it is safe. Imodium is classified as a category C medication. Prescription and over-the-counter drugs are classified by the FDA to reflect how safe or hazardous they are during pregnancy. A category c medication is in the middle and falls into the gray area. There may have been some risk of harm to a fetus in animal studies, but there are no controlled pregnancy trials to assess the safety of category C medications. The general rule with most category C medications is that the benefits should outweigh any potential hazards. Pregnant women, on the other hand, should not make this decision on their own. They should instead consult with their doctor, who will advise them on the best course of action.

Imodium A-D Interactions

  • Cholestyramine
  • Bethanechol
  • Cisapride
  • Metoclopramide
  • Erythromycin

Imodium Dosage Forms

Imodium comes in the following formulations

  • Caplets are capsule-shaped tablets that help with indigestion.
  • Softgels are liquid-filled capsules that help with indigestion.
  • Oral solution is a liquid that is used to treat indigestion.
  • Imodium Multi-Symptom Relief caplets are capsule-shaped tablets that treat a variety of symptoms

References

https://www.medicalnewstoday.com/articles/imodium#how-it-works
https://www.medicalnewstoday.com/articles/imodium#fa-qs
Lomotil vs. Imodium: Differences, similarities, and which is better for you
https://www.fda.gov/drugs/drug-safety-and-availability/fda-limits-packaging-anti-diarrhea-medicine-loperamide-imodium-encourage-safe-use
https://www.imodium.com/anti-diarrhea-medicine
https://www.medicinenet.com/loperamide/article.htm#which_drugs_or_supplements_interact_with_loperamide
https://www.rxlist.com/imodium-drug.htm#description
Taking Imodium While Pregnant: What You Need to Know
https://www.imodium-me.com/how-does-imodium-work
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Loperamide
Medicines

Loperamide: Uses, Mechanism of Action and Warnings

by Healthlinear
written by Healthlinear

What is Loperamide?

Used to treat non-specific diarrhea, Loperamide; an anti-diarrheal long-acting drug is also a suitable candidate for the treatment of Chronic diarrhea or gastroenteritis. It is an OTC (over-the-counter) oral anti-diarrheal medication that was initially introduced in 1969. It was first used medically in 1976 and became available as a non-prescription medicine in 1988.

What is Loperamide used for?

Presently, the FDA has approved this drug for the treatment of numerous types of diarrhea, and it is also used off-label to treat diarrhea caused by chemotherapy. Non-medical use of the drug has grown in popularity in recent years, with applications ranging from self-management of opiate withdrawal effects to euphoria induction (getting high). A novel illness known as loperamide-induced cardiotoxicity has just been discovered. When it is used in toxic levels, patients might develop a variety of potentially lethal dysrhythmias.

Loperamide Mechanism of Action

Loperamide operates through a variety of methods to reduce peristalsis and fluid secretion, leading to a prolonged gastrointestinal transit time and higher fluid and electrolyte absorption from the gastrointestinal tract. It's a phenylpiperidine analog with a molecular structure comparable to diphenoxylate and haloperidol, which are opiate receptor agonists. The drug works by directly inhibiting peristaltic activity in the circular and longitudinal muscles of the intestinal wall. It binds to opioid mu-receptors and is a non-selective calcium channel blocker.

Pharmacokinetics

Loperamide is an agonist for the mu-receptor. CYP3A4, a cytochrome P450 enzyme, extracts it in the liver and metabolizes it. It is conjugated after that and eliminated in the bile. There is almost no active loperamide in the systemic circulation at recommended doses.

It has less than 2% bioavailability. Its onset of action is almost 1 hr, with a plasma half-life of almost 11 hours. The unaltered loperamide and its metabolites are mostly excreted in the feces.

Available Dosage Forms

Loperamide is available in the following different dosage forms:

  • Oro-dispersible tablets
  • Capsules
  • Tablets
  • Syrup

Loperamide Dosage

Traveler’s diarrhea or acute diarrhea

The initial recommended dose is 4mg

The subsequent dose is 2mg after every unformed stool (total dosage should not exceed 8mg per day OTC, and with prescription, maximum dosage per day limit is 16mg)

Loperamide Side Effects

Following are some undesirable effects:

  • Urinary retention
  • Fecal impaction
  • Ileus
  • Dizziness and drowsiness
  • Dry mouth and constipation
  • Other serious side effects associated with the use of the drug are toxic megacolon, necrotizing enterocolitis, toxic epidermal necrolysis, syncope, Stevens-Johnson syndrome, Syncope, Torsade de pointes, Ventricular tachycardia, Ventricular tachycardia, and Cardiac arrest.

Overdose

CNS effects can develop in children under the age of two who are given large amounts, or in children who have accidentally overdosed.

How to reverse undesirable effects produced by Loperamide?

Undesirable effects of the drug can be reversed by using Naloxone.

Loperamide Warnings

Loperamide contraindications are given below:

  • Children less than two years old
  • Bloody diarrhea
  • Acute ulcerative colitis,
  • Diarrhea related to bacterial infections

Why Loperamide is banned?

In recent times, there has been a considerable increase in the use and misuse of the drug as a manner of self-management of withdrawal symptoms and as a cheap way to produce euphoria or to achieve a euphoric mood. People have been using it to self-medicate to reduce the withdrawal symptoms of opiate addiction or to speed up the tapering process. High-dose loperamide has recently shown potential in this regard.

So, FDA has limited packaging for anti-diarrhea medication loperamide HCL (Imodium) to encourage safe use.

Indications

FDA approved uses of the drug Loperamide include

  • Various types of diarrhea such as traveler’s diarrhea
  • Irritable bowel syndrome (IBS) is associated with chronic diarrhea
  • Acute nonspecific diarrhea in patients two years of age and older
  • Decreasing ileostomy output
  • Chemotherapy-related diarrhea

Interactions

It shows interactions with the following drugs

  • Erythromycin
  • Fluconazole
  • Ketoconazole
  • Quinidine
  • Ritonavir

Loperamide Hydrochloride Brand Names

Is Loperamide the same as Imodium?

Yes. This drug is sold over the counter (OTC), under the brand name Imodium. Imodium contains Loperamide HCL as the active ingredient.

Is it safe to take Loperamide (Imodium) during pregnancy

Taking Loperamide during pregnancy may be said okay but there are no shreds of evidence. FDA classifies the drug as a Pregnancy Category C drug. A drug classified as category C medication is in the middle and falls into the gray area. There could be some risk of harm to a fetus in animal studies, but there are no controlled pregnancy trials to assess the safety of category C medications.

Reference

https://pubmed.ncbi.nlm.nih.gov/18192961/
https://go.drugbank.com/drugs/DB00836
https://doi.org/10.1016/j.jpainsymman.2011.06.001
https://www.fda.gov/drugs/drug-safety-and-availability/fda-limits-packaging-anti-diarrhea-medicine-loperamide-imodium-encourage-safe-use
https://www.ncbi.nlm.nih.gov/books/NBK557885/
Taking Imodium While Pregnant: What You Need to Know
https://www.sciencedirect.com/science/article/pii/S0885392411002636
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