Leki diseases test 1. | Quizlet

Civemeline class of drug MOA

direct parasympathomimetics

MOA: activation of muscarinic receptors

Civemeline Indications, SE

I: Glaucoma, Sjorgen syndrome, xerostomia, antidote in poisoning with parasympatholytics

SE: nausea, vomitting, diaphoresis, salivation, bronchocontriction

Neostigimine class of drug, MOA

Indirect parasympathomimetic

MOA: reversible inhibition of acetylcholinesterase → ↑ concentration of acetylcholine at receptors of cholinergic synapses

Neostigmine Indications

postoperative bowel or bladder atony,

glaucoma,

myasthenia gravis,

reversal of neuromuscular blockade caused by non depolarizing muscle relaxants,

antidote in poisoning with parasympatholytics

Donepezil class of drug, MOA

Indirect parasympathomimetic

MOA: reversible inhibition of acetylcholinesterase → ↑ concentration of acetylcholine at receptors of cholinergic synapses

Donepezil indications

Alzheimer's disease, dementia

Umeclidinium class of drug, MOA

Parasympatholytic

Has increased selectivity for M3 receptors

Umeclidinum indications

Treatment of chronic obstructive pulmonary disease (COPD)

Solifenacin class of drug, MOA

parasympatholytic

Has increased selectivity for M3 receptors

Solifenacin indications

Urinary incontinence (specifically, overactive bladder)

Pralidoxime class of drug, MOA

Reactivator

It works by reactivating the phosphorylated acetylcholinesterase (AChE) by binding to the organophosphate

Pralidoxime indications

used as an antidote, for example, in organophosphate poisoning

Atropine class of drug, MOA

Parasympatholytic (cholinolytic)

MOA: It prevents acetylcholine (ACh) from acting as a neurotransmitter at muscarinic receptors8. It is also used as an antidote to counterbalance the peripheral muscarinic effects of organophosphate poisoning

Atropine indications, SE

Indications:

-Premedication before anaesthesia to avoid mucus hypersecretion (bronchial secretion)

-Treatment of bradycardia and AV blocks

-Prevention of cardiac arrest

SE:

-hyperthermia

-mydriasis

-dry mouth, inhibition of glandular secretion

-flushing/redness

-disorientation, hallucinations, motor restlessness, central nervous system effects

-Other peripheral side effects include tachycardia and constipation

Antidote for atropine overdose

Pilocarpine

Physostigmine

Xylometazoline class of drugs

Alpha-sympathomimetic (specifically, an α1-adrenergic receptor agonist)

Xylometazoline indications, SE

Indications:

-Used as a topical decongestant, commonly available as an over-the-counter nasal spray11.

Side effects:

-Prolonged use can lead to rhinitis medicamentosa

Prazosin class of drugs

Selective alpha1-sympatholytic

Prazosin indications, SE

Indications:

Benign Prostate Hyperplasia11

Side effects:

Orthostatic hypotension

Tachycardia

Vertigo

Sexual dysfunction

Dizziness and drowsiness

Headache

Nasal congestion

Tamsulosin class of drug, MOA

Class:

Uroselective alpha1A-sympatholytic11.

Mechanism of action:

It lowers the tonus of smooth muscle in the prostatic region

Tamsulosin indications

Benign Prostate Hyperplasia, where it helps improve micturition with minimal effect on blood pressure

Fenoterol class of drugs

Selective beta2-sympathomimetic (a short-acting beta2 agonist)

Fenoterol indications

Asthma

Bronchospasm

Bronchitis

Chronic obstructive pulmonary disease (COPD)13

Prevention from premature delivery or miscarriage

Salmeterol class of drug

Selective beta2-sympathomimetic (a long-acting beta2 agonist)

Salmeterol indications

Asthma

Bronchospasm

Bronchitis

Chronic obstructive pulmonary disease (COPD)

Indacaterol class of drug

Selective beta2-sympathomimetic (an ultra-long-acting beta2 agonist)

Indacaterol indications

Asthma

Bronchospasm

Bronchitis

Chronic obstructive pulmonary disease (COPD)

Timolol class of drug

Beta-sympatholytic (a non-selective beta-blocker, Ist generation)

Timolol indications

Glaucoma

Angina pectoris

Atrial fibrillation & cardiac arrhythmias

Hypertension

Congestive heart failure

Myocardial infarction

Propranolol class of drug

Beta-sympatholytic (a non-selective beta-blocker, Ist generation)

Propranolol indications

Migraine

"Scenic fear" (performance anxiety)

Angina pectoris

Atrial fibrillation & cardiac arrhythmias

Hypertension

Congestive heart failure

Myocardial infarction

Sotalol class of drug

Beta-sympatholytic (a non-selective beta-blocker, Ist generation)

Carvedilol class of drug

Beta-sympatholytic (a IIIrd generation beta-blocker)

Nebivolol class of drug

Beta-sympatholytic (a IIIrd generation beta-blocker)

Methyldopa class of drug, MOA

Antiadrenergic (specifically, an α2-adrenergic receptor agonist)

It crosses the blood-brain barrier and is converted to alpha-methyldopamine and then to alpha-methyl-norepinephrine

Methyldopa indications, SE

Indications:

High blood pressure in pregnancy

Side effects:

Fatigue

Orthostatic hypotension

Hepatic damage

Immune haemolytic anaemia

Pantoprazole class of drugs, MOA

Proton pump inhibitor

MOA: It inhibits gastric acid production by blocking the H+/K+-adenosine triphosphatase enzyme system (the proton pump) of the gastric parietal cell

Pantoprazole indications

Gastric ulcers

Gastro-duodenal erosions

Used in combination with antibacterial drugs to eradicate H. pylori

Gastric acid reduction during general anaesthesia17

Gastro-oesophageal reflux disease (GERD)1718

Structuring and erosive oesophagitis

Pantoprazole SE

Nausea

Abdominal pain

Constipation

Flatulence

Diarrhoea

Famotidine class of drug, MOA

H2 receptor inhibitor

It inhibits acid production by reversibly competing with histamine for binding to H2 receptors on the basolateral membrane of parietal cells

Famotidine indications, SE

Indications:

To promote healing of gastric and duodenal ulcers

To treat uncomplicated GERD

To prevent the occurrence of stress ulcers

Adverse effects:

Diarrhoea

Constipation

Fatigue

Drowsiness

Headache

Misoprostol class of drug MOA

Prostaglandin analogue

It is a synthetic analogue of prostaglandin E1 which inhibits gastric acid secretion, causes vasodilatation in the submucosa, and stimulates the production of protective mucus

Misoprostol indications, SE

Indications:

Healing and prophylaxis of gastric and duodenal ulceration in patients on NSAID therapy

Adverse effects:

Diarrhoea

Abdominal pain

Nausea and vomiting

Dyspepsia

Flatulence

Abnormal vaginal bleeding

Rashes

Dizziness

Anthraquinones class of drug, MOA

Laxatives

They act by damaging epithelial cells. They affect large intestine motility, resulting in accelerated colonic transit (thus reducing fluid absorption), and affect secretion processes, resulting in enhanced fluid absorption. At a cellular level, a main target is the inhibition of the Cl−-channels across colon cells. The aglycones are hydrolysed by colonic bacteria enzymes

Anthraquinones indications, SE

Indications:

Temporary constipation

Notes: The effect typically occurs after 6-8 hours and acts in the large intestines

Adverse effects:

Melanosis coli

Diarrhoea

Abdominal pain

Anthraquinones examples

Physicon

Chrysophanol

Aloe-emodin

Rhein

Sennosides

Bisacodyl class of drug, MOA

Laxative

It works by stimulating parasympathetic nerve endings in the colonic mucosa. The active form stimulates the myenteric plexus (nerve cells in the gut wall), increasing peristaltic movements and accelerating colonic transit. It is hydrolysed by intestinal enzymes (in the small and large intestines) and by colonic bacteria (in the large intestines).

Bisacodyl indications, SE

Indications:

To relieve occasional constipation and irregularity

For short-term relief of constipation24

To prepare the bowel for medical procedures (such as colonoscopy) when thorough bowel cleansing is required

Notes: The effect occurs after 6-10 hours when acting in the small and large intestines, or 6-8 hours when acting in the large intestines

Adverse effects:

Diarrhoea

Abdominal pain (mainly in the upper abdomen)

Flatulence

Headache

Prucalopride class of drug, MOA

5-HT4 receptor agonist

It enhances the release of acetylcholine from enteric neurons, which promotes gastrointestinal motility and accelerates gastric emptying and intestinal transit

Prucalopride indications, SE

Indications:

Chronic Idiopathic Constipation

Irritable Bowel Syndrome with Constipation

Symptoms such as nausea and bloating associated with delayed gastric emptying

Adverse effects:

Diarrhoea

Abdominal pain

Nausea

Bloating

Headache

Dizziness

What can Cisapride (5-HT4 receptor agonist) cause?

QT prolongation, can increase the risk of severe arrhythmias

Loperamide class of drug, MOA

antidiarrheal (Opioid Receptor Agonist)

Primarily acts on the mu-opioid receptors in the gut to slow intestinal motility. It has a high affinity for peripheral opioid receptors, leading to effective diarrhoea control without central nervous system (CNS) effects.

Loperamide indications, SE

Indications:

Acute diarrhoea

Chronic diarrhoea

Traveller's diarrhoea

Side effects

Constipation

Dizziness

Abdominal discomfort

Racecadotril class of drug, MOA

Antidiarrheal

It is a prodrug that is converted in the body to thiorphan, an inhibitor of intestinal enkephalinase

Racecadotril indications, SE

Indications:

Acute diarrhoea in infants and children over 3 months of age.

Adverse effects:

Headaches

Erythema

Rash

Hydroxyzine class of drug, MOA

First-generation antihistamine (H1 receptor antagonist)

Inverse agonist at histamine H1 receptors; also has sedative and anxiolytic effects via CNS action

Hydroxizine indications, SE

Indications:

Anxiety and tension associated with psychoneuroses,

allergic conditions causing pruritus and urticaria, sedation before/after anesthesia,

nausea and vomiting (excluding pregnancy-related)

Side Effects:

Drowsiness, dry mouth,

rare serious effects include QT prolongation,

heart rhythm changes, allergic reactions

Loratadine: Class and MOA

Second-generation antihistamine (H1 receptor antagonist).

Selective peripheral H1 receptor antagonist; minimal CNS penetration.

Loratadine: Indications and Side Effects

Indications:

Allergic rhinitis,

urticaria,

allergic skin conditions.

Side Effects:

Headache,

dry mouth,

fatigue,

minimal sedation.

Betahistine: Class and MOA

Histamine analogue (H1 receptor agonist and H3 receptor antagonist). Increases histamine release by antagonizing H3 receptors; improves inner ear blood flow.

Betahistine: Indications and Side Effects

Indications:

Vertigo, Ménière's disease, vestibular disorders.

Side Effects:

Headache,

nausea,

GI discomfort,

rare allergic reactions.

Pitolisant: Class and MOA

Histamine H3 receptor antagonist/inverse agonist. Blocks H3 autoreceptors, increasing histamine release and promoting wakefulness.

Pitolisant: Indications and Side Effects

Indications:

Narcolepsy with or without cataplexy.

Side Effects:

Insomnia,

headache,

nausea,

anxiety.

Ondansetron: Class and MOA

5-HT3 receptor antagonist. Blocks serotonin 5-HT3 receptors centrally and peripherally to prevent nausea/vomiting.

Ondansetron: Indications and Side Effects

Indications: Prevention/treatment of chemo-, radiation-, and surgery-induced nausea/vomiting.

Side Effects:

Headache,

constipation,

dizziness,

QT prolongation (rare).

Sumatriptan: Class and MOA

Serotonin 5-HT1B/1D receptor agonist (triptan). Vasoconstriction of cranial vessels; inhibits pro-inflammatory neuropeptides.

Sumatriptan: Indications and Side Effects

Indications:

Acute migraine and cluster headache treatment.

Side Effects:

Tingling,

flushing,

dizziness,

chest tightness,

rare cardiovascular events.

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