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Propranolol | A Beta-Adrenergic Receptor Antagonist

propranolol inderal

 

IntroductionPropranolol, available under the brand name of Inderal is  a non-selective beta adrenergic antagonist is used to treat a variety of conditions, including hypertension, angina, atrial fibrillation, myocardial infarction, migraine, essential tremor, and hypertrophic subaortic stenosis.
PharmacodynamicsPropranolol belongs to a beta-adrenergic receptor antagonist is used to treat hypertension. Given once or twice daily, depending on the indication, propranolol has a long duration of action. Patients who quit taking propranolol abruptly risk worsening of their angina and myocardial infarctions.
The S(-)-enantiomer of propranolol, a racemic combination of two enantiomers, has roughly 100 times the binding affinity for beta adrenergic receptors than the R(-)-enantiomer. 9 The most prevalent illness for which propranolol is prescribed is hypertension.
Mode of ActionNonselective beta-adrenoreceptor antagonist Propranolol is also categorized as a class II antiarrhythmic. It responds by competitively blocking the heart’s normal epinephrine and norepinephrine-induced beta-1 and beta-2 adrenergic activation.

On cardiac myocytes, including the sinoatrial and atrioventricular nodes, there are beta-1 receptors. These receptors are activated, which results in an increase in cyclic AMP and an increase in intracellular calcium. Increased muscle fiber contractility results from this mechanism. Beta-adrenergic receptor blockade causes the heart’s overall workload to be reduced, which in turn lowers oxygen consumption and causes myocardial remodeling. [8]
On the other hand, beta-2 receptor activation results in an increase in cyclic AMP, which activates protein kinase A and causes smooth muscle cells in many organs and arteries to relax. Therefore, there is a slight vasoconstriction when beta-2 receptors are inhibited. Due to this action, it can be difficult for asthmatics to administer emergency epinephrine since it prevents epinephrine from potentially binding to pulmonary receptors. [9] Beta-blockers have a Vd of approximately 4 to 6 L/kg and are well distributed throughout the body. They are also highly protein-bound.

IndicationsHypertension can be treated with propranolol. Additionally, myocardial infarction, atrial fibrillation, migraine, essential tremor, hypertrophic subaortic stenosis, pheochromocytoma, and proliferating infantile hemangioma are all conditions for which propranolol is prescribed.
Availability & UsageBeta-blockers are processed mostly in the liver, like the majority of drugs ( both the active and inactive compounds). Due to first-pass metabolism in the hepatic circulation, only around 25% of the medicine consumed enters the systemic circulation.

Propranolol’s active metabolite, 4-hydroxypropranolol, is created via hydroxylation with the help of the CYP2D6 enzyme.
Additionally, propranolol, like the majority of ingested drugs, is primarily eliminated by the kidneys, having a half-life of between 3 and 6 hours in people with healthy renal systems.

You can administer propranolol intravenously or orally. Continuous ECG monitoring should be done while a gradual infusion is administered intravenously. This method of administration is most frequently used in inpatient settings.

The dosage of propranolol varies, mainly depending on the ailment it is used to treat.

Side EffectsBradycardia, gastrointestinal problems, abdominal pain, nausea, erectile dysfunction, and wheezing/bronchospasms are some of the most typical side effects of using propranolol. Use of propranolol may also result in weariness, drowsiness, and cold extremities. Hallucinations, insulin resistance, and allergic reactions are a few severe side effects to be aware of. Before writing a propranolol prescription for a patient, prescribers must go over all the side effects with them.
Drug Interation
(while taking with other medicine)
Important WarningIn some cases, propranolol may result in heart failure. If you experience chest pain or discomfort, dilated neck veins, intense exhaustion, erratic breathing, an irregular heartbeat, swelling of the face, fingers, feet, or lower legs, or weight gain, consult your doctor immediately once.
Available BrandsInderal

 

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Atenolol | A Second-Generation beta-1-selective adrenergic antagonist

 

IntroductionAtenolol, available under brand names of Tenormin, Blokium, Zafnol is Synthetic beta-1 selective blocker. Atenolol is used to treat hypertension, chronic angina, and to lower mortality in individuals with known or suspected myocardial infarction who are hemodynamically stable.
Class of MedicineAtenolol is a second-generation beta-1-selective adrenergic antagonist lowers myocardial contractility, blood pressure, and heart rate.
Mode of ActionBecause it selectively binds to the 1-adrenergic receptor as an antagonist up to a reported 26 fold more than 2 receptors, atenolol is a cardioselective beta-blocker. 15 Due to the greater population of this receptor in cardiac tissue, selective action at the 1 receptor results in cardioselectivity. Therapeutic doses can still cause some binding to 2 and potentially 3 receptors, but the effects caused by antagonising these receptors are greatly diminished compared to those caused by non-selective drugs. Due to the Gs coupling between the 1 and 2 receptors, inhibiting their activation decreases the activity of adenylyl cyclase and the downstream signalling that it produces via cyclic adenosine monophosphate and protein kinase A.
PKA is hypothesised to mediate the activation of ryanodine receptors and L-type calcium channels in cardiomyocytes by phosphorylating these proteins. The release of calcium from the sarcoplasmic reticulum (SR) and an increase in contractility can then be caused by the 16 L-type calcium channels, which can first cause an increase in intracellular calcium. By phosphorylating phospholamban, which in turn enhances the SR Ca2+ ATPase’s affinity to promote calcium reuptake into the SR, PKA also contributes to the termination of contraction. Additionally, it phophorylates troponin I to lessen the protein’s affinity for calcium. Both of these occurrences result in a contraction reduction, which when combined with the initial contraction increase, enables faster cycling and, as a result, a higher heart rate with increased contractility.
PKA is hypothesised to mediate the activation of L-type calcium channels and ryanodine receptors in cardiomyocytes by the phosphorylation of these proteins. The ryanodine receptors are then triggered to release calcium that has been held in the sarcoplasmic reticulum (SR), leading to enhanced contractility, after an initial spike in intracellular calcium is provided by 16 L-type calcium channels. The phosphorylation of phospholamban by PKA, which enhances the SR Ca2+ ATPase’s affinity to promote calcium absorption into the SR, contributes to the termination of contraction as well. In order to lessen troponin I’s affinity for calcium, it also phophorylates the protein. When combined with the initial rise in contraction, both of these occurrences result in a contraction reduction, enabling faster cycling and, as a result, a greater heart rate with increased contractility.
IndicationsA second-generation beta-1-selective adrenergic antagonist called atenolol is used to treat acute myocardial infarction, angina pectoris, and hypertension. Treatment of arrhythmias, migraine prevention, paroxysmal supraventricular tachycardia, alcohol withdrawal, thyrotoxicosis prevention, and prophylaxis against subsequent myocardial infarction are only a few of the non-FDA authorised uses. In cases of infantile hemangiomas, atenolol may also be used instead of propranolol, though further study is necessary before use.
Avaiability & UsageFor oral treatment, atenolol comes in 25 mg, 50 mg, and 100 mg tablets; 0.5 mg/mL is also available for intravenous injection. Depending on the indication, a different dosage and administration method is used.

Hypertension
Atenolol’s starting dose for adults is 50 mg per day, either either as a single tablet or along with diuretic medication. After a few weeks, if there hasn’t been a significant therapeutic response, the dosage may be increased to one 100 mg tablet taken once daily. Higher daily doses are unlikely to result in additional advantages.  If the patient has a creatinine clearance of less than 15 ml/min, a lower dose of 25 mg per day may be utilised for elderly or renally impaired patients. Before giving them a new dose, careful blood pressure monitoring is required.

Chronic chest pain
The initial adult dose for non-vasospastic angina is 50 mg once daily. One 100 mg pill should be used each day if, after a week, the patient has not had the best results. For the best therapeutic outcome, some patients could require 200 mg per day. The patient should be observed and told to reduce their physical activity during this period since withdrawal should be accomplished gradually. [

Myocardial Infarction Acute
Within 12 hours after the myocardial infarction, intravenous injection should take place as soon as the patient enters the hospital.

For instance, the FDA advises giving an adult a 5-minute IV atenolol injection followed by a 10-minute IV injection of another 5-mg dose. After 12 hours, an oral dose of 50 mg should be taken. Then, for the following 6 to 9 days or until the patient is discharged from the hospital, oral dose might be either 50 mg twice daily or 100 mg once daily.

Migraine Prevention
The initial adult dose is 25 mg once daily, which is increased to 100 mg once daily over the course of 1-2 weeks.

T-wave supraventricular rhythm
The first dose of atenolol for adults, as recommended by the ACC and AHA, is 25 to 50 mg per day, which is increased to 100 mg once daily based on tolerance and response.

Coronary infarction
Most patients should begin taking beta-blockers within 24 hours of their myocardial infarction, and they should continue taking them for secondary prophylaxis, gradually increasing their dose up to 50 mg twice day depending on their blood pressure, heart rate, and side effects.

Thyrotoxicosis
The initial dose is 25–50 mg once daily, which is increased as necessary to a maximum of 100 mg twice daily in order to treat tachycardia, palpitations, and trembling.

Employing in the Particular Patient Populations
Patients with hepatic impairment: The manufacturer’s labelling does not mention changing the dosage. Additionally, as was already mentioned, atenolol undergoes very little hepatic metabolism.
Patients with Impairment of Renal Function: Patients with impaired renal function should be watched closely, and the dose has to be changed in accordance with creatinine clearance.
No dose change is required if creatinine clearance is more than 30 mL/min.
Creatinine clearance 10–30 mL/min: 50 mg/day as the maximum dose.
Maximum dose up to 25 mg per day for creatinine clearance 10 mL/minute.
Those undergoing hemodialysis Hemodialysis effectively removes atenolol; provide atenolol after hemodialysis.

Considerations for Pregnancy:
Former FDA pregnancy category D drug is atenolol. [19] Atenolol is not advised during pregnancy, under the recommendations of The American College of Obstetricians and Gynecologists (ACOG), due to the possibility of growth restriction and low birth weight. Labetalol is the chosen beta blocker for pregnant women with persistent hypertension.

Considerations When Breastfeeding: Plasma protein binding is primarily responsible for the excretion of beta blockers in breast milk Drugs like atenolol (10% PPB), which have low plasma protein binding, are extensively excreted in breast milk.

Side EffectsThe following are atenolol’s side effects, per the product label.

Avoid stopping atenolol suddenly because doing so could make your angina, acute myocardial infarction, or ventricular arrhythmias worse. It is advised that the dose be reduced gradually.
It is advised that atenolol be swiftly reintroduced briefly if angina worsens or acute coronary insufficiency develops.
Bradycardia, dizziness, constipation, confusion, dyspnea, headaches, erectile dysfunction, nausea, lethargy, paraesthesia, peripheral numbness, rash, sleep disturbances, syncope, visual impairment, and bronchospasm are a few of the more typical adverse effects.
Alopecia, dry mouth, postural hypotension, psychosis, psoriasis, thrombocytopenia, depression, moderate transaminitis, and depression are uncommon adverse reactions.
Severe bradycardia, renal failure, atrioventricular blockage, shock, and hyperkalemia are the traits of the BRASH syndrome. If you suspect BRASH syndrome, stop taking atenolol.

Drug Interaction
CautionIn some cases, atenolol may result in cardiac failure. If you experience discomfort or pain in your chest, consult a doctor right once; Swelling of the face, fingers, feet, or lower legs; dilated neck veins; extreme fatigue; irregular breathing; an irregular heartbeat; weight gain; or wheezing
Available BrandsTenormin
Blokium
Zafnol

 

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Duloxetine | SNRI | Anti-Depressant

IntroductionDuloxetine available under brand names of Dulan, Duron, Cymbalta is used off-label for conditions like stress incontinence and peripheral neuropathy brought on by chemotherapy. Major depressive disorder (MDD), generalised anxiety disorder (GAD), fibromyalgia, diabetic peripheral neuropathy, and chronic musculoskeletal pain are all conditions that can be treated with duloxetine.
Class of MedicineIt belongs to the group of drugs known as SNRIs, or serotonin and norepinephrine reuptake inhibitors. This activity explains the benefits of duloxetine as a treatment for a variety of illnesses, how it works, and when it should not be used.
Mode of ActionDuloxetine treats depression and anxiety by inhibiting serotonin and norepinephrine reuptake, integrating two therapeutic processes in a single drug. Additionally, dopamine levels in the prefrontal brain are raised by duloxetine. The blockage of norepinephrine transporters is the mechanism of action for the rise in dopamine levels. These transporters are able to function on both dopamine and norepinephrine because they have a strong affinity for dopamine. As a result, blocking norepinephrine transporters may result in a rise in dopamine. The prefrontal cortex, which lacks dopamine transporters and mainly relies on norepinephrine transporters for reuptake, is the location of this surge in dopamine.
Duloxetine works to treat depression and anxiety by inhibiting the reuptake of serotonin and norepinephrine. This combines two therapeutic methods into a single medication. Duloxetine raises dopamine levels in the prefrontal cortex as well. Norepinephrine transporters are inhibited as part of the mechanism of action for the rise in dopamine levels. The fact that these transporters can function on both dopamine and norepinephrine is due to their high affinity for dopamine. Inhibiting norepinephrine transporters can therefore result in a rise in dopamine. The prefrontal cortex, which has less dopamine transporters and a higher reliance on norepinephrine transporters for reuptake, is where this surge in dopamine is concentrated.
Medical UsesIbuprofen is a common pain reliever used to treat a variety of aches and pains, such as back pain, period pain, and toothache. It also helps with inflammation from strains and sprains, as well as arthritis discomfort. It comes in the form of tablets, capsules, and a syrup that you ingest.
Avaiability & UsageDue to its excellent oral absorption, duloxetine is most frequently administered in capsules, either with or without food. It is not advised to chew or crush duloxetine. Duloxetine, however, may hold its stability for up to two hours after being opened and sprinkled on apple juice or apple sauce, according to tests.

Treatment for fibromyalgia:
30 mg taken once day for a week, followed by an increase to 60 mg taken once daily. Another option is to use a titration strategy, starting with a dose of 20 mg per day and gradually increasing it by 20 mg each week, up to 60 mg, as tolerated. The daily maximum is 60 mg.
Treatment for generalised anxiety disorder (GAD): The starting dose is 60 mg, but depending on the patient’s tolerance, the dose may be reduced to 30 mg once daily for a week before being increased to 60 mg once daily. Increasing doses above 60 mg/day have been reported to offer benefits by certain experts, despite research showing no extra benefits.
Treatment for unipolar major depressive disorder (MDD): A single dose of 40 to 60 mg/day or two divided doses are both acceptable. It might be essential to start with 30 mg/day for a week before increasing the dosage to 60 mg/day. 60 milligrammes per day for maintenance.

Initially, 60 mg can be given to treat the pain brought on by diabetic peripheral neuropathy; however, depending on the patient, lower starting doses may be more suitable. The daily maximum is 60 mg.

Chronic musculoskeletal pain treatment:
Low back pain: As an adjuvant therapy, 30 mg can be used once daily for a week before being increased to 60 mg once day as tolerated. The daily maximum is 60 mg.

Knee pain:
When an additional therapy, 30 mg once day for a week can be administered, and as tolerated, up to 60 mg once daily

Side EffectsCommon adverse effects of duloxetine include:

Headache
Drowsiness
Fatigue
Nausea
Xerostomia
Abdominal pain
Weight loss
Weakness
Insomnia
Dizziness
Chane in libido
Diaphoresis
Constipation
Decreased appetite
Tremor
Diarrhea
Erectile dysfunction

Caution
(while taking with other medicine)		Patient Pregnant
Due to the FDA pregnancy category C of duloxetine, there is a possibility of danger to foetal development. Duloxetine showed negative effects on embryo/fetal development in animal reproduction studies. As a result, the doctor should only recommend duloxetine if the advantages outweigh the possible risks to the foetus.Women Who Breastfeed
Duloxetine can have affects on breastfeeding infants because it is secreted in breast milk. The relative infant dose (RID) of duloxetine, according to certain research, is 2.3%. When compared to the mother’s dose, the RID is the dose consumed by breast milk. Breastfeeding is acceptable with a RID of less than 10%. Some sources state that if the mother is taking psychiatric medication, nursing should only be encouraged if the RID is less than 5%.

Nevertheless, it is important to keep an eye out for behavioural changes, sleep disturbances, feeding abnormalities, growth, and neurodevelopment in a baby who is nursed by a woman who uses duloxetine .[7]

Elderly
Numerous instances of clinically severe hyponatremia in older persons are correlated with the use of SSRIs and SNRIs. Duloxetine should only be prescribed with caution to elderly patients. However, it is not necessary to change the dosage based on the patient’s age .[8]

Important WarningDeaths have resulted from dosages as low as 1000 mg. Serotonin syndrome, seizures, coma, somnolence, syncope, tachycardia, autonomic instability, diarrhoea, and vomiting are all indications of an overdose. Agitation, restlessness, confusion, diaphoresis, heat, tachycardia, nausea, vomiting, tremor, rigidity of the muscles, hyperreflexia, myoclonus, dilated pupils, dry mucous membranes, and increased bowel noises are all symptoms of serotonin syndrome. Serotonin syndrome is particularly prone to clonus and hyperreflexia.

An overdose of duloxetine cannot be reversed. Cyproheptadine and cooling techniques may be utilised if the patient has serotonin syndrome. Patients with aberrant vital signs require observation, and serious instances can necessitate ICU-level treatment.

Available BrandsDulan
Duron
Cymbalta

 

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Fluconazole | An Antifungal Triazole

fluconazole

 

IntroductionFluconazole, available under brand names of Zolanix, Fungone, Triazoline is a triazole antifungal is used to treat a variety of fungal infections, such as candidiasis, blastomycosis, coccidiodomycosis, cryptococcosis, histoplasmosis, dermatophytosis, and pityriasis versicolor. Fluconazole, also referred to as Diflucan, is an antifungal medication used to treat superficial and systemic fungal infections in a range of tissues.
Class of MedicineFluconazole is an antifungal triazole class . It functions by inhibiting the development of infection-causing fungus.
Mode of ActionA fluorine-substituted bis-triazole antifungal agent is called fluconazole. Similar to other azoles, it works by attaching to fungal cytochrome P-450 and then disrupting fungal membranes, which prevents lanosterol from being converted to ergosterol.
The fungus (or yeast) that is causing the infection is eliminated by fluconazole. The medication kills the fungus by rupturing the cell membrane and allowing the insides to escape. Your symptoms will improve as a result of this treatment for the infection.
Medical UsesCandida infection is treated and prevented using fluconazole. An infection with one of the various varieties of the fungus Candida is what causes this illness. Vaginal yeast infection and oral yeast infection are two examples of candidiasis (thrush).

Additionally, infections in your throat, oesophagus, lungs, and blood can be brought on by candidiasis. Fluconazole may be used to treat bone marrow transplant recipients in order to prevent candidiasis. This is due to the fact that their immune systems are compromised, which increases their risk of contracting a severe form of candidiasis.

Infection of the brain and spinal cord brought on by the fungus Cryptococcus is similarly treated with fluconazole.

Avaiability & UsageFluconazole is available in the following dosage forms and doses:

Oral Tablet: 50 mg, 100 mg, 150 mg, 200 mg.
IV Solution (Injection): 200 mg/100 ml, 400 mg/200 ml, 100 mg/50 ml.
Liquid Suspension: 200 mg/100 ml, 400 mg/200 ml, 100 mg/50 ml.

Fluconazole must be administered multiple times to treat a fungus, with the exception of vaginal candidiasis. Based on how the patient reacts to the treatment, the dose is changed. Until the infection is entirely cured, be sure to periodically consult the doctor to assess the effectiveness of the therapy.
The following is a list of fluconazole dosages that are suggested for specific conditions:
Vaginal Candidiasis: One oral dose of 150 mg.
Those who have oropharyngeal and esophageal candidiasis may begin treatment with a dose of 200 mg the first day, followed by 100 mg once each day.

200 mg the first day for Candida peritonitis, then 50 to 200 mg once daily after that.
Infections of the urinary tract: 200 mg the first day, then 50 to 200 mg once daily.
Blood Candida Infections: 400 mg daily maximum.
Up to 400 mg/day for the prevention of fungal infections (candidiasis) in patients receiving bone marrow transplants.

Side EffectsThe most frequent adverse effect of fluconazole administration is sleepiness, along with the following effects:

Headache.
Diarrhea.
Nausea or abdominal pain
Vomiting.
A significant rash appears on people with weakened immune systems.
Among the damaging side effects include
Liver Damage: The following signs and symptoms could indicate that your liver is damaged.
Whites of the eyes or skin become yellow.
Rough skin.
Sickness or vomiting
Torsions with points: (a life-threatening heartbeat condition).
Symptoms consist of
Irregular, quick heartbeat.
Fainting and dizziness
Seizures.

Caution
(while taking with other medicine)		Before using fluconazole, tell your doctor if any of the following problems exist:

Allergy: Previous history of allergy to fluconazole or any other azole-class drugs.

Fluconazole might be harmful to the foetus if used during pregnancy and while nursing. Therefore, let your doctor know if you plan to become pregnant or plan to breastfeed during the first three months of your pregnancy. The doctor could suggest using birth control during treatment and for a week after the last dose to prevent pregnancy.

Heart Diseases: Let your doctor know if you have a history of heart illness, especially if you have an irregular heartbeat or low potassium levels. This is due to the fact that fluconazole has been linked to alterations in heartbeat. Consequently, precautions should be made before giving the drug.

Skin Rashes: Contact your doctor right away if any skin rashes appear after using this medication.

Surgery: Before having any type of surgery, including dental surgery, tell your doctor that you’ve been taking fluconazole.

Endocrine Issues: Fluconazole has been linked to alterations in the quantities of hormones generated by the adrenal glands. Once the medicine is stopped, this is reversible, and the levels revert to normal.

Important WarningAdrenal gland issues could result from this medication. If you have diarrhoea, dizziness, fainting, lack of appetite, mental depression, nausea, skin rash, unusual tiredness or weakness, or vomiting, consult your doctor immediately once.
Available BrandsZolanix,
Fungone
Triazoline

 

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Levosulpiride | A Prokinetic Agent

IntroductionLevosulpiride avaiable under the brand of Levopraid, is an atypical antipsychotic medication. It is used to treat psychiatric disorders such as depression, schizophrenia, vertigo, and hallucinations. However, it can also be used to treat digestive issues such as GERD, IBS, indigestion, and chronic heartburn. It is also prescribed by doctors to prevent premature ejaculation.
Class of MedicineLevosulpride | A Prokinetic Agent,  belongs to the antipsychotic medication class (also known as neuroleptics or tranquillizers). It is mostly used to treat hallucinations, schizophrenia, bipolar disorder, anxiety, and vertigo, among other mental illnesses.
Mode of ActionThe main mechanism of action of levosulpiride is to block the D2 dopaminergic receptors, which are preferentially located on the presynaptic membranes in the brain’s dopaminergic pathways; this means that sulpiride is a selective autoreceptor blocker.
Medical UsesLevosulpiride is used to treat the following conditions:

Psychosis
Schizophrenia’s negative symptoms
Anxiety problems
Dysthymia
Vertigo
Dyspepsia
Irritable bowel syndrome (IBS)
Ejaculation occurs too soon.
In the United Kingdom and other European countries, levosulpiride is not currently approved for the treatment of premature ejaculation.

Avaiability & UsageLevosulpride is available in tablet form. Should be taken only on your doctor’s prescription. Take LEVOSULPIRIDE with or without food. The tablet form of LEVOSULPIRIDE should be swallowed as a whole, do not crush, or break the tablet.
Side EffectsPatients taking levosulpiride frequently experience the following side effects:

Amenorrhea is the absence of menstrual periods.
Gynecomastia is a condition in which men’s breasts become enlarged.
Changes in sex motivation
Galactorrhea is the discharge of milk from the nipples when a woman is not breastfeeding.
If levosulpiride is not taken as directed, it can cause serious health problems.

The following are rare but serious side effects:

A potentially fatal condition characterised by a high fever
Breathing and heart rate are both fast.
Pulse irregularity
Confusion
Sweating
Neuroleptic malignant syndrome is characterised by a significantly altered mental state.

Important WarningPatients with a history of neuroendocrine tumours, epilepsy, manic states, abnormally high levels of prolactin in the blood, painful, lumpy breasts, heart disease, any allergy, and during pregnancy and breastfeeding should exercise caution.
Available BrandsLevopraid

 

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Itopride | A Gastroprokinetic Agents

IntroductionItopride, marketed under the brand name of Ganaton, ITP, Nogerd and more, is a prokinetic benzamide derivative. Itopride is a dopamine D2 receptor antagonist and acetylcholine esterase inhibitor that is used to treat symptoms of functional dyspepsia such as nausea and vomiting.
Class of MedicineITOPRIDE HYDROCHLORIDE belongs to a class of drugs known as ‘gastroprokinetic agents, gastrokinetic agents, or propulsives,’ which are primarily used to treat disorders associated with decreased gastrointestinal motility.
Mode of ActionItopride has both anticholinesterase (AchE) and dopamine D2 receptor antagonistic activity. M3 receptors are well known to exist on the smooth muscle layer throughout the gut, and acetylcholine (ACh) released from enteric nerve endings stimulates smooth muscle contraction via M3 receptors. The enzyme AChE hydrolyzes the released ACh, inactivating it and thus inhibiting gastric motility, resulting in a variety of digestive problems. Dopamine, in addition to ACh, is found in significant amounts in the gastrointestinal tract and has several inhibitory effects on gastrointestinal motility, including the reduction of the lower esophageal sphincter and intragastric pressure. These effects appear to be mediated by the D2 subtype of dopamine receptors and appear to result from suppression of ACh release from myenteric motor neurons. Itopride removes the inhibitory effects of dopamine D2 receptor antagonism on Ach release. It also inhibits the enzyme AchE, preventing ACh degradation. The net result is an increase in ACh concentration, which promotes gastric motility, raises lower esophageal sphincter pressure, speeds up gastric emptying, and improves gastro-duodenal coordination. Itopride’s dual mode of action is distinct and distinct from the actions of other prokinetic agents on the market.
Medical UsesItopride is typically used to treat GI symptoms caused by decreased GI motility: non-ulcer/dysmotility dyspepsia (gastric “fullness”, discomfort, and possible pain)
Gastroparesis (delayed gastric emptying)
Anorexia
Heartburn \Sregurgitation
Other possible gastric, prolactin, or dopamine-related conditions include bloating, nausea, and vomiting.
In placebo-controlled trials, itopride was shown to significantly improve symptoms in patients with functional dyspepsia and motility disorders.These studies concluded that itopride was significantly superior to placebo in terms of reducing the severity of symptoms of functional dyspepsia after 8 weeks of treatment, and that itopride yielded a higher rate of response than placebo in terms of significantly reducing pain and fullness.
Avaiability & UsageITOPRIDE HYDROCHLORIDE tablets are available in 50mg and 100mg strengths. Based on your medical condition, your doctor will advise you on how frequently you should take ITOPRIDE HYDROCHLORIDE.
The usual dose is 50mg tab twice daily or 150mg once daily.
Side EffectsItopride’s most common side effects are mild to moderate
Abdominal pain
Diarrhoea
Rashes
Giddiness
Exhaustion
Back or Chest pain
Increased Salivation
Constipation
Headache
Sleeping disorders
Dizziness
Galactorrhea
GynecomastiaBecause of poor penetration across the blood brain barrier, adverse effects on the central nervous system are rare, though a slight increase in prolactin levels may occur. Prolactin levels are more likely to rise when taking itopride at high doses.
Important WarningItopride can cause leukopenia, or a decrease in the normal level of white blood cells, which can be fatal.
Available BrandsGanaton
ITP
Nogerd

 

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Azithromycin | a Macrolide Antibiotic

 

IntroductionAzithromycin available under brand names of Azomax, Macrobac, Azitma, Zetro and more, is a macrolide antibiotic with a long half-life and a high level of tissue penetration.

It is primarily used to treat respiratory, enteric, and genitourinary infections, but it can also be used to treat some sexually transmitted and enteric infections in place of other macrolides. It has a similar structure to erythromycin 2.

Class of MedicineAzithromycin is a type of antibiotic known as a macrolide antibiotic. It works by either killing or preventing the growth of bacteria. This medication, however, will not help with colds, flu, or other virus infections.
Mode of ActionBacteria require a specific process of protein synthesis, which is enabled by ribosomal proteins, in order to replicate. Azithromycin binds to the bacterial 50S ribosomal subunit’s 23S rRNA. It inhibits protein synthesis in bacteria by inhibiting the transpeptidation/translocation step as well as the assembly of the 50S ribosomal subunit. Labeling As a result, various bacterial infections are controlled. Label number seven. The high affinity of macrolides for bacterial ribosomes, including azithromycin, is consistent with their broad spectrum antibacterial activity.

Azithromycin is highly stable at low pH, giving it a longer serum half-life and higher tissue concentrations than erythromycin.

Medical UsesAzithromycin should only be used to treat or prevent infections caused by susceptible bacteria, in order to prevent the development of antimicrobial resistance and maintain the efficacy of azithromycin Label.

Azithromycin is used to treat patients who have mild to moderate infections caused by susceptible strains of the microorganisms listed in the specific conditions below. Dosages, duration of therapy, and considerations for different patient populations may differ between these infections.

Avaiability & UsagePneumonia in the Community
Indicated for the treatment of community-acquired pneumonia caused by Chlamydophila pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae, or Streptococcus pneumoniae in patients who can take oral antibiotics.Day 1: 500 mg PO x 1 dose, followed by 250 mg PO then OD on 2-5 DaysTonsillitis or Pharyngitis
Indicated as an alternative therapy for Streptococcus pyogenes-caused pharyngitis/tonsillitis in patients who are unable to receive first-line therapy.Day 1: 500 mg PO x 1 dose, followed by 250 mg PO then OD 2-5 Days.

Skin/skin structure that is uncomplicated
Indicated for the treatment of uncomplicated Staphylococcus aureus, Streptococcus pyogenes, or Streptococcus agalactiae skin and skin structure infections.

Day 1: 500 mg PO x 1 dose, followed by 250 mg PO then Daily on Days 2-5.

Exacerbations of chronic obstructive pulmonary disease caused by acute bacterial exacerbations
Acute bacterial exacerbations of chronic bronchitis caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae are indicated for treatment.

OR 500 mg PO qDay for 3 days

Alternatively, on Day 1, take 500 mg PO x 1 dose, followed by 250 mg PO qDay on Days 2-5.

Bacterial sinusitis, acute
Acute bacterial sinusitis caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae is treated with this medication.

500 mg PO Daily for three days

Chancroid Indicated for the treatment of genital ulcer disease in men caused by Haemophilus ducreyi (chancroid)

The efficacy of chancroid treatment in women has not been established.

1 dose of 1000 mg PO

Urethritis and Cervicitis caused by nongonococcal or gonococcal bacteria
It is used to treat urethritis and cervicitis caused by Chlamydia trachomatis or Neisseria gonorrhoeae.

1 dose of 1000 mg PO

Inflammatory Pelvic Disease
Indicated in patients requiring initial IV therapy for pelvic inflammatory disease caused by Chlamydia trachomatis, Neisseria gonorrhoeae, or Mycoplasma hominis.

Side EffectsThese common side effects of azithromycin happen in more than 1 in 100 people. There are things you can do to help cope with them:

Feeling sick (nausea)
Diarrhoea
Being sick (vomiting)
Losing your appetite
Headaches
Feeling dizzy or tired
Changes to your sense of taste
Keep taking the medicine, but talk to your doctor or pharmacist if these side effects bother you or do not go away.

Serious side effects
Serious side effects are rare and happen in less than 1 in 1,000 people.

Call your doctor right way if:

You have a faster or irregular heartbeat (arrhythmia)
the whites of your eyes turn yellow, or your skin turns yellow (this may be less noticeable on brown or black skin), or you have pale poo with dark pee – these can be signs of liver or gallbladder problems
You get ringing in your ears (tinnitus), temporary hearing loss, or you feel unsteady on your feet (vertigo)
You have severe pain in your stomach or back – this can be a sign of inflammation of the pancreas (pancreatitis)
You have diarrhoea (perhaps with muscle cramps) that contains blood or mucus – if you have severe diarrhoea without blood or mucus for more than 4 days you should also speak to a doctor

Important WarningA word about the dangers of liver toxicity:
Because azithromycin is primarily eliminated by the liver, caution should be exercised when administering azithromycin to patients with impaired hepatic function.

A word about possible renal toxicity:
Because there is a lack of data in patients with renal GFR less than 10 mL/min, caution should be used when prescribing azithromycin to these patients.

Available BrandsAzomax
Macrobac
Azitma
Zetro

 

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Clarithromycin | A Macrolide Antibiotic

clarithromycin town pharmacy
IntroductionClarithromycin available under the brand names of Klaricid, Claritek, Clarion and more, is an antibiotic that can be used to treat a variety of infections.
It’s used to treat chest infections like pneumonia, as well as skin diseases like cellulitis and ear infections.
Helicobacter pylori, a bacteria that can cause stomach ulcers, is also treated with it.People who are allergic to penicillin and antibiotics that are related to penicillin, such as amoxicillin, may take clarithromycin.
Class of MedicineClarithromycin belongs to the macrolide antibiotics family of drugs. It works by preventing bacteria from growing. Colds, flu, and other viral diseases will not respond to antibiotics like clarithromycin.
Mode of ActionBy attaching to the bacterial 50S ribosomal subunit, clarithromycin, a semisynthetic macrolide antibiotic derived from erythromycin, suppresses bacterial protein production. Binding prevents amino acid translocation during translation and protein assembly by inhibiting peptidyl transferase activity.
Medical UsesClarithromycin is used to treat bacterial infections such pneumonia, bronchitis (infection of the tubes that lead to the lungs), and infections of the ears, sinuses, skin, and throat.
Avaiability & UsageClarithromycin in gernerally available in Tablet and Syrup forms.

Indicated for the treatment of mild-to-moderate infections caused by susceptible isolates of Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, or Streptococcus pneumoniae.

For 7-14 days, take 250-500 mg every 12 hours.

1000 mg once daily for 7 days (extended release)

Acute Sinusitis of the Maxilla
Indicated for the treatment of mild to severe infections caused by Haemophilus influenzae, Moraxella catarrhalis, or Streptococcus pneumoniae susceptible isolates.

For 14 days, take 500 mg every 12 hours.

1000 mg once daily for 14 days (extended release)

Infection with Mycobacterium
Treatment and prophylaxis for mycobacterial infections are recommended.

For 7-14 days, take 500 mg every 12 hours.

Use in combination with other antimycobacterial medications to treat disseminated infection caused by Mycobacterium avium complex (MAC) (eg, ethambutol)

Peptic Ulcer Disease (PUD) is a type of stomach ulcer.
When treating individuals with active or history of peptic ulcer disease, this medication is recommended for H pylori eradication.

For 10-14 days, take 500 mg every 8-12 hours.

Administer with bismuth subsalicylate, amoxicillin, H2 receptor antagonist, or proton pump inhibitor as part of a 2- or 3-drug combination therapy.

Tonsillitis, Pharyngitis: 250 mg every 12 hours for 10 days

Pneumonia acquired in the community
Susceptible isolates of Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, Streptococcus pneumoniae, or Chlamydophila pneumoniae are used to treat mild to moderate illnesses.

For 7-14 days, take 250 mg every 12 hours.

1000 mg once daily for 7 days (extended release)

250 mg every 12 hours for 7-14 days for skin/skin structure infection

Pertussis is a kind of pertussis that causes (Off-label)
Off-label use for pertussis treatment or post-exposure prophylaxis

For 7 days, take 500 mg PO twice a day.

Side EffectsGeneral Side Efeects in more than 1%
Gastrointestinal (GI) effects, general (13%)
Abnormal taste (adults, 3-7%)
Diarrhea (3-6%)
Nausea (adults, 3-6%)
Vomiting (adults, 1%; children, 6%)
Elevated blood urea nitrogen (BUN; 4%)
Abdominal pain (adults, 2%; children, 3%)
Rash (children, 3%)
Dyspepsia (2%)
Heartburn (adults, 2%)
Headache (2%)
Elevated prothrombin time (PT; 1%)
Caution
(while taking with other medicine)		Heart and Blood Vessel Problems.

In patients with these conditions, clarithromycin may increase the risk of heart and blood vessel problems. It could happen a year or ten years after taking this medication. If you are concerned about this risk, consult your doctor. This medication may cause diarrhoea, which can be severe in some cases.

Important WarningClarithromycin may cause QT prolongation, which is a heart rhythm problem. This condition can result in rapid, erratic heartbeats. Clostridium difficile-associated diarrhoea can be caused by almost all antibiotics, including clarithromycin.
Available BrandsKlaricid
Claritek
Clarion

 

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Ibuprofen – NSAID – An Everyday Pain Killer

IntroductionIbuprofen available under brand name of Brufen is a common pain reliever used to treat a variety of aches and pains, such as back pain, period pain, and toothache. It also helps with inflammation from strains and sprains, as well as arthritis discomfort.
Class of MedicineIbuprofen belongs to the NSAID (nonsteroidal anti-inflammatory drug) class of drugs. It works by inhibiting the creation of a chemical that causes pain, heat, and inflammation in the body
Mode of ActionIbuprofen is a non-selective inhibitor of cyclooxygenase (COX), an enzyme essential for prostaglandin synthesis via the arachidonic acid pathway. COX is required for the conversion of arachidonic acid to prostaglandin H2 (PGH2). After then, PGH2 is converted to prostaglandins. As a result of ibuprofen’s suppression of COX, the body’s production of prostaglandins is reduced.

PGH2 produces prostaglandins, which are key mediators of feelings like pain and inflammatory processes including fever and inflammation. Ibuprofen’s antipyretic effects may be due to its influence on the hypothalamus, which results in vasodilation, increased peripheral blood flow, and subsequent heat dissipation.

Medical UsesIbuprofen is a common pain reliever used to treat a variety of aches and pains, such as back pain, period pain, and toothache. It also helps with inflammation from strains and sprains, as well as arthritis discomfort. It comes in the form of tablets, capsules, and a syrup that you ingest.
Avaiability & UsageIbuprofen is available in form of Tablet, Syrup and Cream (for external use)

Adults should take one or two 200mg pills three times each day. If necessary, your doctor may prescribe a larger dose of up to 600 mg to be taken four times each day. This should only be done under the guidance of a physician.
Allow at least 6 hours between doses if you take ibuprofen three times a day. Allow at least 4 hours between doses if you’re taking it four times a day.

If you’re in constant pain, ask your doctor about slow-release ibuprofen tablets or capsules. These are usually taken once or twice a day in the evening. If you’re taking ibuprofen twice a day, wait 10 to 12 hours between doses.

Ibuprofen tablets or capsules should be swallowed whole with a glass of water or juice. Ibuprofen tablets and capsules should be taken after a meal or snack, or with a glass of milk. It will be less prone to cause stomach discomfort.

Side EffectsMore than 1 in 100 people experience the common negative effects of ibuprofen taken by mouth. If these side effects annoy you or don’t go away, talk to your doctor or pharmacist:

headaches
feeling nauseous
feeling unwell (nausea)
being unwell (vomiting)
wind \sindigestion

Caution
(while taking with other medicine)		Some drugs don’t combine well with ibuprofen.

When ibuprofen is applied to the skin rather than taken by mouth, it is less likely to interact with other medications.

Before taking ibuprofen or applying it to your skin, tell your doctor if you’re taking any of the following medications for your safety:

    • Warfarin, for example, is a blood thinner.
    • Aspirin, diclofenac, mefenamic acid, and naproxen are anti-inflammatory pain relievers.
  • high blood pressure medications
  • Betamethasone, dexamethasone, hydrocortisone, and prednisolone are examples of steroid medications.
  • Ciprofloxacin, levofloxacin, moxifloxacin, nalidixic acid, norfloxacin, or ofloxacin are examples of antibiotics.
  • Citalopram, fluoxetine, fluvoxamine, venlafaxine, paroxetine, or sertraline are examples of antidepressants.
  • Gliclazide, glimepiride, glipizide, and tolbutamide are examples of diabetes medications.
Important WarningIf you have any of the following symptoms, see a doctor right away.

  • Swollen ankles
  • Blood in your pee, or not peeing at all – these can be indicators of a kidney problem.
  • Black poo or blood in your vomit – these can be signs of stomach bleeding.
  • Severe chest or stomach discomfort – this could indicate a hole in your stomach or gut, as well as trouble breathing or worsening asthma symptoms.
Available BrandsBrufen

 

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Metformin | Biguanide | Anti-diabetic

IntroductionMetformin, marketed under the trade names Glucophage, Neophage, Neodipar and others, is the first-line treatment for type 2 diabetes, particularly in overweight people. It’s also used to treat polycystic ovarian syndrome (PCOS).  It is taken by mouth and is not linked to weight gain. It’s sometimes used as an off-label supplement to help persons who take antipsychotics and phenelzine avoid gaining weight.
Class of MedicineMetformin belongs to a group of medicines known as biguanides. Metformin aids in the regulation of glucose (sugar) levels in the blood. It reduces the amount of glucose you receive from food as well as the quantity of glucose your liver produces.
Mode of ActionThe mechanisms of action of metformin are distinct from those of other oral antihyperglycemic medications. Metformin lowers blood glucose levels by reducing hepatic glucose synthesis (gluconeogenesis), lowering glucose absorption in the intestine, and improving insulin sensitivity by enhancing peripheral glucose uptake and utilisation Label. Metformin is widely known for inhibiting mitochondrial complex I activity, and it has long been assumed that this is how it achieves its effective anti-diabetic actions 6,11. The actions described above result in a drop in blood glucose, which helps to manage type 2 diabetes and improve glycemic control.
Medical UsesMetformin is a drug that is used to treat and prevent type 2 diabetes in those who are at a high risk of developing it. Metformin is used to treat polycystic ovarian syndrome (PCOS), despite the fact that it isn’t officially approved for the condition.
Avaiability & UsageMetformin is available as tablet, and extended-release (long-acting) tablet for oral administration. The standard tablet is usually taken two or three times a day with meals. The extended-release tablet is normally taken with dinner once a day. Take metformin at the same time(s) every day to help you remember to take it.
Follow the directions on your prescription label carefully, and if there is anything you don’t understand, ask your doctor or pharmacist to explain it to you. Metformin should be used exactly as prescribed. Do not take more or less of it, or take it more frequently than your doctor has suggested.
Side EffectsMetformin, like all drugs, can produce adverse effects, though not everyone experiences them.

Side effects that are common:
More than 1 in 100 people have common side effects.

If these side effects annoy you or do not go away after a week, talk to your doctor or pharmacist:

feeling unwell (nausea)
diarrhoea or getting sick (vomiting)
stomach pains
a decrease in appetite
In the mouth, there is a metallic taste.

Important WarningMetformin use is strongly discouraged in some individuals whose kidneys do not function normally because it increases the chance of developing lactic acidosis, a dangerous and potentially fatal condition in which too much lactic acid builds up in the blood.
Available BrandsGlucophage
Neophage
Neodipar