Heartburn is a painful burning sensation experienced in the upper stomach or chest area due to the reflux of stomach acid in the esophagus.
The reflux is triggered usually by poor diet and lifestyle which causes the lower oesophageal sphincter (LES) to relax and give way to flow the acid backward.
Though heartburn is a relatively common disorder and can be treated with simpler drugs, its negligence can lead to the development of a more severe and chronic condition called gastro-oesophageal reflux disease (GERD) [1].
Prescription Drugs
Prescription drugs, as the name suggests, are those medications which are prescribed by the doctor or a medical practitioner and are not available in the market without a written instruction [2].
They are strictly prescribed and not freely available because they could be of use in a specific condition and might have adverse effects if taken without a doctor’s advice due to their tendency to either react with food substances, drinks, other ongoing medicines or due to their tendency to exacerbate the effects of certain unrelated medical condition already present in the patient.
They are instructed by the doctor on a written note with a symbol Rx which in Latin means recipe meaning “to take” [3],[4].
Types of Prescription Drugs used for Heartburn Treatment
There are a number of drugs prescribed by the doctors to treat heartburn. The chemical composition for them is generally common in most of them, what differs is their label which is different according to the brand.
Most common prescription drugs fall into two types namely histamine type 2 receptor blockers/antagonists, proton pump inhibitors and pro-motility agents.
Histamine type 2 Receptor Antagonists
H2 blockers/antagonists are those compounds that bind and block the histamine type 2 receptors in the parietal cells of the gut.
Antagonizing these cell receptors interferes and inhibits the acid production in the stomach, thereby, reducing the symptoms of heartburn.
The selectivity of H2 blockers is of utmost importance as they have no effect if they block a similar receptor called histamine Type1, which is a target of anti-histamines to block allergic reactions and which does not inhibit acid secretion [5].
There are majorly 4 types of H2 antagonistic compounds that can be taken for heartburn namely famotidine, nizatidine, ranitidine and cimetidine.
There are a number of prescription and non-prescription drugs available which contain either one of these or a combination of these chemicals.
H2 receptor blockers are usually slow in their action (take approximately 30-90 minutes to show an effect) but once active, their effectiveness is very long lasting.
There are a number of capsules or tablets available in the market with prescription which has to be taken by mouth often before the first meal of the day.
In some cases they can also be taken before an evening meal in which case, it would be directed by the doctor.
If the symptoms don’t seem to improve at all after a few weeks of consumption or any other unwanted symptoms are observed, the doctor should be contacted immediately [6].
Proton Pump Inhibitors
Proton pump inhibitors are one of the most effective means of reducing chronic heartburn or gastro-oesophageal reflux disease where all lines of medications fail.
They work by blocking the proton pumps in the gastric cells by binding to K+/H+ ATPase pumps which control the final step in the production of gastric acid.
Like H2 inhibitors, proton pump inhibitors also act slowly but the effect is long-lasting.
The reason why they are more efficient than H2 blockers is that they have high selectivity and specificity in the gut, which makes their actions more efficacious [7].
They are available in the form of tablets or capsules which are to be swallowed and not chewed with water.
The major chemical compounds that form the constituents of most PPI tablets are omeprazole, esomeprazole, lansoprazole, rabeprazole, pantoprazole, and dexlansoprazole.
Since they are the strongest of all heartburn medications and can have unwanted effects on the body, their dosage is supposed to be very precise and mostly for up to maximum 2-4 weeks [8] .
Promotility agents
The above two types of medications for acid reflux essentially reduced the secretion of acid in the stomach to prevent its reflux.
However, the probability agents do not block acid secretion but increase the motility of the gut so that the acid is emptied faster into the intestine and out.
This prevents the acid to be trapped in the gut for long, which otherwise would have stayed there and caused reflux.
Promotility agents are rarely given for heartburn as low motility is not usually the case of occurrence of heartburn.
The most widely studies chemicals with these activities are bethanechol, cisapride, metoclopramide, and domperidone.
They work either by enhancing the excitatory neurotransmitter acetylcholine action of by blocking an inhibitory neurotransmitter such as dopamine.
With the exception of cisapride, the actions of the other three are not widely studied [9].
Examples of Major Prescription Drugs Available for Heartburn
1. Nizatidine Capsule
It is an H2 blocker containing nizatidine as an active ingredient. It is taken by swallowing 1 tablet (with a concentration of 150 mg) with a glass of water twice a day.
The dose should not be exceeded beyond two tablets in 24 hours without a prescription.
It is given up to 8 weeks up till the treatment of symptoms and then it is taken in a dose of 150 mg once per day as maintenance therapy [10].
2. Fluxid
It contains famotidine as an active ingredient. It is also an H2 blocker and should be taken in a dose of 1 tablet by keeping on the tongue as it is absorbed in the system automatically after disintegration which takes about 2 minutes.
It doesn’t need any fluid for swallowing. For children above 12 years and adults, the ideal dose is 40 mg to be taken once during bedtime and for maintenance, 20 mg a day at bedtime [11].
3. Pepcid
Having famotidine as its content, Pepcid is an H2 antagonistic agent. Pepcid is indicated for short term treatment in patients with GERD and gastric ulcers.
The recommended oral dose in adults is 20 mg for up to six weeks and for those with chronic heartburn including ulceration and oesophageal erosion, the dose is followed up to 12 weeks.
For pediatric patients of ages 1-16 years, the dose kept is 2 mg/kg/day [12].
4. Cimetidine Hydrochloride
It contains cimetidine as an active ingredient and is an H2 blocker. It is available in the form of syrups and is used to treat diagnostically (via endoscopy) confirmed GERD.
The recommended dose is 1200 mg divided in a day (800 mg two times or 400 mg 4 times) for 12 weeks to heal heartburn and maintain the effects.
The results of the use of cimetidine beyond 12 weeks have not been established [13].
5. Aciphex
It contains rabeprazole sodium which is a proton pump inhibitor. Aciphex is indicated for short term administration (4-8 weeks) for healing and symptomatic relief from gastro oesophageal reflux disease.
For adults over 12 years of age, it can be taken in the dose of 1 capsule (20 mg) with or without a glass of water every 24 hours for 8 weeks. The capsule should never be chewed or crushed.
The course can be repeated for another 8 weeks if the symptoms don’t resolve. For less severe GERD, the recommended adult oral dose is 1 aciphex 20 mg delayed-release tablet to be taken once daily for four weeks [14].
6. Dexilant
A proton pump inhibitor, dexilant contains dexlansoprazole as its active ingredient. The recommended dose for adults of dexilant is for up to 8 weeks which is indicated for healing all grades of heartburn.
It is indicated to maintain relief from heartburn for up to 6 months. It is to be taken just before meals to prevent and relieve the symptoms of acid reflux or as indicated by the doctor.
Dexilant is available in the capsules of 30 and 60 mg strengths for adult use and should be taken as prescribed depending on the severity of the symptoms [15].
7. Nexium
It contains esomeprazaole magnesium which again is a proton pump inhibitor.
Nexium is indicated for the short term treatment (4-8 weeks) for healing diagnostically approved GERD in adults and children above 1 year of age.
Dexilant is available as capsules of 10, 20 and 40 mg strength for children and adult use and should be taken as prescribed depending on the severity of the symptoms [16].
8. Protonix
A tablet containing pantoprazole sodium, protonix is indicated in adults and pediatric patients 5 years of age and older for short term treatments (up to 8 weeks) in the healing of acid reflux.
For those adult patients who have not healed after 8 weeks of treatment, an additional 8 week course may be considered but its safety beyond that has not been researched on.
Protonix is indicated for the maintenance of gastro oesophageal reflux disease and reduction in relapse rates of daytime and nighttime heartburn symptoms in adult patients for up to 12 months.
It is supplied in tablets and in oral suspensions with concentrations of 20 and 40 mg to be taken [17].
9. Esomeprazole Strontium
It is a proton pump inhibitor containing esomeprazole. It is indicated for short term treatments (4-8 weeks) of symptomatically confirmed heartburn. the recommended dose is 24.65 mg once daily for 4 weeks.
The dose can be increased in case of severe non-responsive heartburn or erosive oesophagitis.
If the symptoms do not heal by short term treatment, the course can be repeated for another 4 weeks. For maintenance of healing, it is given once daily for no more than 6 months [18].
10. Omeprazole
Omeprazole delayed-release capsules are indicated for the short term treatment (4-8 weeks) of diagnostically approved heartburn in pediatric and adult patients.
The course can be repeated for another 4 weeks if the symptoms don’t resolve. The efficacy of omeprazole delayed-release capsules used for longer than 8 weeks in patients has not been established.
The recommended adult oral dose for the treatment of patients with symptomatic GERD is 20 mg daily for up to 4 weeks. It should be taken 10-60 minutes before meals or as indicated by the doctor [19].
11. Metozolv ODT
It is a metoclopramide hydrochloride tablet, which is a pro-motility agent.
Metozolv ODT is indicated as short term (4-12 week) therapy for adults with symptomatic and diagnostically approved GERD who fail to respond to conventional therapy.
It is taken by mouth on an empty stomach before at least 30 minutes of eating as food can decrease its concentration in blood.
It is an orally disintegrating tablet and is taken in a dose of 10-15 mg four times a day. The dose shouldn’t be exceeded beyond 12 weeks.
It comes with being able to cause tardive dyskinesia in some patients which is a serious motility disorder and often irreversible [20].
Side effects and Precautions
There are different side effects and precautions for each drug which are indicated by the doctor. Possible side effects of H2 receptor antagonists include headache, constipation, diarrhoea, nausea, and vomiting.
Proton pump inhibitors can also have the same set of side effects including upset stomach and abdominal pain. PPIs may also increase the chances of getting an infection in intestines and for making the bones fragile.
These side effects, however, are very rare. Promotility agents may have major rare but major side effects and any appearance of unusual symptoms on their consumption should be reported immediately.
Precautions of heartburn drugs are indicated specifically by the doctor and should be strictly followed.
The doctor should be told about every past or present medical condition including pregnancy and breastfeeding before taking the prescription.
If a dose is missed, it should not be replaced by two doses at the same time or taking the tablet at an odd time (between the indicated intervals) [21].
Summary
Heartburn drugs are commonly prescribed by medical practitioners and are generally effective and safe to use.
They provide a long term effect as compared to antacids and other over the counter medications for the treatment of acid reflux. However, each tablet has its own effects and can be dangerous if the indicated doses are not followed.
It is important to abide by the given course of medication strictly and any unusual problem faced during administration should be reported immediately to avoid any future discomfort.