Block 3 drugs Flashcards
How do antiemetic antihistamines work ?
-Antiemetic antihistamines are a class of medications used to treat nausea, vomiting, and dizziness caused by motion sickness. Although vomiting is considered to be a protective reflex action of the body to expel toxic substances in the stomach and gut, antiemetic medications are often necessary to suppress vomiting, especially to prevent dehydration.
Antiemetic antihistamines work in the following ways:
-Vomiting is controlled by the vomiting center in the brain, which is activated by triggers such as strong smell, thoughts, and motion.
-Antiemetic agents bind to the receptors in the vomiting center of the brain stem and block their signaling pathways (that lead to nausea and vomiting), thus reducing the nausea sensation.
-The inner ear plays a key role in maintaining balance; antiemetic antihistamines desensitize the inner ear to the motion of the head and reduce the inner ear’s ability to sense motion.
-In addition, they produce a calming effect on the brain that leads to slight drowsiness.
Chlorpromazine
Drug class:
H1 receptor antagonist
Contraindications:
- Chlorpromazine should be avoided in patients with hypothyroidism, phaeochromocytoma, myasthenia gravis and prostate hypertrophy. It should be avoided in patients known to be hypersensitive to phenothiazines
side effects:
- agitation
- dizziness
Chlorpromazine ( Phenothiazine) (antiemetic)
Drug class:
-Dopamine D2-receptor antagonist
- they also have blocking action at muscarinic and histamine receptors.
What is dystonia ?
-Dystonia is a medical term for a range of movement disorders that cause muscle spasms and contractions. The spasms and contractions may either be sustained or may come and go. Movements are often repetitive and cause unusual, awkward and sometimes painful postures.
Cyclizine
- anti - sickness medication / antiemetic
Side effects:
- feeling drowsy
- dry mouth
- blurred vision
- headaches
- constipation
Mechanism: Cyclizine is a histamine H1 receptor antagonist
How do H1 receptor antagonists work ?
- When the CTZ (chemoreceptor trigger zone) is stimulated, vomiting may occur.
- H1 antagonists have little or no activity against vomiting produced by substances acting directly on the CTZ but are effective in motion sickness and against vomiting caused by substances which act locally in the stomach.
- H1 receptor antagonist are most effective if given before the onset of nausea and vomiting but may have some action in controlling it when established.
- Effects can last for about 24hrs and their peak anti emetic effect occurs after about 4 hrs.
People who shouldn’t take H1 receptor antagonist:
- ever had an allergic reaction to cinnarizine or any other medicine
-porphyria (an inherited blood condition)
-severe liver disease
-problems peeing or emptying your bladder
-epilepsy or any other health problem that causes fits or seizures
-an eye problem called primary angle closure glaucoma
-Parkinson’s disease, as cinnarizine could make your symptoms worse
Cinnarizine
Drug class: antihistamine
Indication: nausea and vomiting due to motion sickness
Mechanism: H1 receptor antagonist
Contraindications:
- Parkinson’s disease ( as cinnarizine can make your symptoms worse)
- liver disease
- if you have an allergy test (cinnarizine affects the results of allergy tests)
Side effects:
- feeling drowsy
- feeling sick
Cinnarizine
- is an antihistamine
- also a calcium channel blockerof the diphenylmethylpiperazine group.
- adults and children aged over 5 years can take it
What are 5-HT antagonists ?
- 5- hydoxytryptamine is released in either the CNS or the gut and is an important neurotransmitter in emesis ( the action or process of vomiting).
- 5- HT3 antagonists for example ondanestron are proving to be a particular value in preventing and treating vomiting caused by cytotoxic drugs.
Ondansetron
Ondansetron is used to prevent nausea and vomiting particularly for controlling the severe nausea and vomiting that occurs with many forms of cancer chemotherapy - a major advance since this is the main reason limiting the effective use of chemotherapy.
- its also effective against gastroenteritis.
- Gastroenteritis is a very common condition that causes diarrhoea and vomiting. It’s usually caused by a bacterial or viral tummy bug
- ondansetron can be taken PO/IM/IV which is useful when a patient is unable to keep food down
Ondansetron
Drug class: antiemetic
Indication: to prevent nausea and vomiting
Mechanism: blocks serotonin (5-HT3) receptors in the chemoreceptor trigger zone (CTZ) and gastrointestinal tract.
Side effects:
- drowsiness
- constipation
- tiredness
- ondansetron can prolong QT interval
Aspirin
- is a nonsteroidal anti-inflammatory drug used to reduce pain, fever, and/or inflammation, and as an antithrombotic.
Ibuprofen
Ibuprofen is a nonsteroidal anti-inflammatory drug that is used for treating pain, fever, and inflammation
Omeprazole (benzimidazole)
Drug class: PPI
Indication: treat teh symptoms of gastrooesphageal disease (GORD)
Mechanism: it irreversibly inhibits H+/K+ - ATPase (the proton pump). This inhibits gastric acid secretion.
Contraindications:
- history of hypersensitivity to the drug
Side effects:
- headaches, feeling sick, stomach pain, constipation
Ompremazole
- proton pump inhibitor
Is a medication used in the treatment of gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome.
- other PPI are lansoprazole and pantoprazole
How do H2 receptor antagonist work ?
- competitively inhibit histamine actions at all H2-receptors, but their main clinical use is as inhibitors of gastric acid secretion.
- H2 receptors antagonist also promote healing of peptic ulcers
Cimetidine
- Cimetidine: H2 receptor antagonist
- Indication:- It is mainly used in the treatment of heartburn and peptic ulcers (stomach ulcers)
-Mechanism: inhibit histamine stimulated and gastrin stimulated acid secretion.
-Is a histamine H₂ receptor antagonist that inhibits stomach acid production.
Side effects:
- hypergastrinemia
- diarrhea
- dizziness
- muscle pains
Cimetidine
- also inhibits cytochrome p450 in the liver and can retard the metabolism of other drugs.
- cimetidine can reduce renal tubular secretion of basic drugs.
Ranitidine
Drug class: antihistamine being used to treat GORD symptoms , treats zollinger Ellison and peptic ulcer disease
Indication: reduce symptoms of GORD
Mechanism: H2 receptor antagonist
Side effects:
-hypergastrinemia
- transient rashes
-muscle pains
- dizziness
- diarrhea
Ranitidine
Ranitidine is not currently available in the UK or globally. It has been discontinued as a precaution because it may contain a small amount of an impurity that has been linked to an increased risk of cancer in animals
- Ranitidine is a medicine that reduces the amount of acid your stomach makes. It was used for indigestion, heartburn and acid reflux, gastro-oesophageal reflux disease (GORD – this is when you keep getting acid reflux), and to prevent and treat stomach ulcers.
-Ranitidine and other H2 receptor antagonists are known to cause gynaecomastia.
- Gynaecomastia (sometimes referred to as “man boobs”) is a common condition that causes boys’ and men’s breasts to swell and become larger than normal. It is most common in teenage boys and older men.
Gaviscon ( alginic acid)
Gaviscon can be used to treat heartburn (acid reflux) and indigestion.
The medicine works by forming a protective layer that floats on top of the contents of your stomach. This stops stomach acid escaping up into your food pipe. Gaviscon also contains an antacid that neutralises excess stomach acid and reduces pain and discomfort.
- best to take Gaviscon after meals and at bedtime.
Gaviscon ( alginic acid)
Indication: for the management of gastric reflux
Mechanism: alginic acid reacts with gastric acid to form a floating “raft” of alginic acid gel on the gastric acid pool. Alginate-based raft-forming formulations commonly contain sodium or bicarbonate; bicarbonate ions are converted to carbon dioxide in presence of gastric acid and get entrapped within the gel precipitate, converting it into a foam which floats on the surface of the gastric contents, much like a raft on water 4. The “raft” has a near neutral pH due to carbon dioxide and floats on the stomach contents and potentially functions as a barrier to impede gastroesophageal reflux
Contraindications:
- children have to be 12 +
Amoxicillin
Drug class: penicillin antibiotic
Therapy Indications: infections caused by gram positive bacteria (especially streptococcal bacteria)
Mechanism:
Amoxicillin competitively inhibits penicillin-binding protein 1 and other high molecular weight penicillin binding proteins.9,10 Penicillin bind proteins are responsible for glycosyltransferase and transpeptidase reactions that lead to cross-linking of D-alanine and D-aspartic acid in bacterial cell walls.10 Without the action of penicillin binding proteins, bacteria upregulate autolytic enzymes and are unable to build and repair the cell wall, leading to bacteriocidal action.
Contraindications:
Side effects: feeling sick/ nauseous
Amoxicillin
Amoxicillin is an antibiotic medication used to treat a number of bacterial infections. These include middle ear infection, strep throat, pneumonia, skin infections, and urinary tract infections among others. It is taken by mouth, or less commonly by injection. Common adverse effects include nausea and rash.
Amoxicillin
Clarithromycin
Clarithromycin, sold under the brand name Biaxin among others, is an antibiotic used to treat various bacterial infections. This includes strep throat, pneumonia, skin infections, H. pylori infection, and Lyme disease, among others. Clarithromycin can be taken by mouth as a pill or liquid
Clarithromycin
Clarithromycin ?
Clarithromycin ?
Clarithromycin ?
Metronidazole
Metronidazole, sold under the brand name Flagyl among others, is an antibiotic and antiprotozoal medication. It is used either alone or with other antibiotics to treat pelvic inflammatory disease, endocarditis, and bacterial vaginosis. It is effective for dracunculiasis, giardiasis, trichomoniasis, and amebiasis
Metrondiazole
Drug class: nitroimidazole antibiotic
Indication:
- treatment of trichomoniasis
- Trichomoniasis is a very common STD caused by infection with Trichomonas vaginalis (a protozoan parasite). Although symptoms vary, most people who have trich cannot tell they have it.
- bacterial vaginosis
Mechanism:
- reduction of metronidazole which is only made by anaerobic bacteria and protozoa, binds deoxyribonucleic acid and electron-transport proteins of organisms, blocking nucleic acid synthesis
Contraindications:
- having dialysis
- cannot be taken whilst drinking alcohol
- liver problems
Side effects:
- Do not drink alcohol while taking the tablets or liquid or using the vaginal gel or suppositories. It can give you severe side effects such as feeling or being sick, stomach pain, hot flushes, difficulty breathing, a pounding heartbeat (palpitations) and headaches.
Metronidazole
- Metronidazole is not a penicillin mediation
dyspepsia
Most people have indigestion (dyspepsia) at some point. Usually, it’s not a sign of anything more serious and you can treat it yourself.
What is the triple therapy option for H pylori infections of the tummy
Metronidazole
Metronidazole
Hyoscine butylbromide
Drug class: Muscarinic receptor antagonist
Indication:Used to treat abdmoninal cramping and pain
Contraindications:
- 6+
- myasthenia gravis
- need to check with your doctor if your preganant
Mechanism: Muscarinic receptor antagonist. butylbromide binds to muscarinic M3 receptors in the gastrointestinal tract 1. This prevents acetycholine from binding to and activating the receptors which would result in contraction of the smooth muscle. The inhibition of contraction reduces spasms and their related pain during abdominal cramping.
Side effects:
- tachycardia
- constipation
- blurred vision
- dry mouth
Hyoscine butylbromide
- Buscopan relieves painful stomach cramps, including those linked with irritable bowel syndrome (IBS).
- Hyoscine butylbromide, also known as scopolamine butylbromide and sold under the brandname Buscopan among others, is an anticholinergic medication used to treat crampy abdominal pain, esophageal spasms, renal colic, and bladder spasms. It is also used to improve respiratory secretions at the end of life
- Buscopan relieves painful stomach cramps, including those linked with irritable bowel syndrome (IBS). It can also help bladder cramps and period pain. Buscopan contains the active ingredient hyoscine butylbromide
- anticholinergic medication
- Buscopan relieves painful stomach cramps, including those linked with irritable bowel syndrome (IBS).
It can also help bladder cramps and period pain.
Buscopan contains the active ingredient hyoscine butylbromide.
It’s not the same as hyoscine hydrobromide, which is a different medicine taken to prevent motion sickness.
Buscopan comes as tablets and is available on prescription. Buscopan also comes as 2 different products that you can buy from a pharmacy or shop:
Buscopan Cramps
Buscopan IBS Relief
It can also be given by injection, but this is usually only done in hospital.
Atorvastatin
Drug class: They are HMG-CoA reductase inhibitors.
Indications: Statins are the first line treatment of high cholesterol.
Mechanism: They are HMG-CoA reductase inhibitors.
This enzyme plays a key role in the production of cholesterol, so inhibiting it reduces the cholesterol in the body.
Side effects: Common side effects of statins include muscle pain, abdominal pain, constipation and headache.
Cholesterol
- Cholesterol is a lipid that can be absorbed from dietary sources or synthesised in the liver.
- It is an essential component of cell membranes allowing them to maintain permeability and fluidity.
-Cholesterol is also required for the production of steroid hormones and fat-soluble vitamins
Cholestrol
Cholesterol
What are proton pump inhibitors ?
Proton-pump inhibitors are a class of medications that cause a profound and prolonged reduction of stomach acid production. They do so by irreversibly inhibiting the stomach’s H⁺/K⁺ ATPase proton pump. They are the most potent inhibitors of acid secretion available.
TB
TB
Rifampicin
Drug class: antibiotic
Indication: for the treatment of TB
Penicillin’s
Pencillin
Tetracyclines
Atorvastatin
Drug class: They are HMG-CoA reductase inhibitors.
Indications: Statins are the first line treatment of high cholesterol.
Mechanism: They are HMG-CoA reductase inhibitors.
This enzyme plays a key role in the production of cholesterol, so inhibiting it reduces the cholesterol in the body.
Side effects: Common side effects of statins include muscle pain, abdominal pain, constipation and headache.
