Block 2 drugs Flashcards by Sana Abbasi

Morphine

Class: Opiate receptor agonist / Analgesic

Indication:
-Morphine is used for the management of chronic, moderate to severe pain.

-cough in terminal diseases

-treatment of opioid dependence

Mechanism of action:
- Morphine-6-glucuronide is responsible for approximately 85% of the response observed by morphine administration.

-Morphine and its metabolites act as agonists of the mu and kappa opioid receptors.

Mimics action of opioid peptide by causing prolonged activation of opioid receptors (mu and kappa), producing analgesia

Contraindications:
- respiratory depression
- chronic lung disease
- Acute kidney
- renal failure

Side effects:
- respiratory depression

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Morphine

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Morphine

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Morphine

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Naloxone

Class: Opiate receptor antgonist

Indication: Opioid overdose, post-operative respiratory depression.

Mechanism of action:

competitive inhibitor of the µ-opioid receptor.

Naloxone antagonizes the action of opioids, reversing their effects.

If a patient has not taken opioids, naloxone does not have a significant effect on patients

Contraindications:
- Cardiovascular disease or those receiving cardiotoxic drugs, physical dependence on opioids (precipitates withdrawal)

Side effects:
- Nausea, vomiting, hypotension, hypertension, ventricular tachycardia and fibrillation, cardiac arrest.

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Naloxone

normal respiratory rate: 12-16 breaths per minute
normal heart rate 60-100 breaths per min

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Naloxone

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Diamorphine

Class: Opiate receptor agonist/Analgesic

Indication:
-Severe pain, cough in terminal disease, adjunct in treatment of opioid dependence.

Mechanism of action:
- binds to my and kappa opioid receptors, prolonging the opiate effect and resulting in analgesia

-More soluble than morphine and so has a more rapid onset of action when given by injection. This also results in more sedation, when compared to morphine.

Contraindications:

-Phaeochromocytoma (tumour of the adrenal glands)

-Acute respiratory deprssion

Side effects:
Nausea (less than morphine), vomiting, respiratory depression, euphoria/mental detachment, abdominal pain, anorexia, hypertension, hypotension (less than morphine), taste disturbance.

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Oxygen

Class: Oxygen therapy

Indication:
Long-term treatment (>15h/day) in patients with severe COPD, severe chronic asthma, CF, obstructive sleep apnoea.

Short burst oxygen therapy (10-20 minutes) in patients who suffer episodes of breathlessness.

Ambulatory oxygen therapy (generally <4h/day) is prescribed to patients who are on long-term oxygen therapy who need to be away from home on a regular basis.

Mechanism of action:
Oxygen therapy in severe acute asthma increases the P(O2) in the air and therefore encourages more oxygen to bind to haemoglobin in the blood, increasing the oxygen saturation levels.

Contraindications:
Smoking during oxygen use. COPD

Side effects:
Hot flushes, vaginal bleeding/discharge, suppression of menstruation, gastrointestinal disturbances, headache, light-headedness, decreased platelet counts.

Normal partial pressure of oxygen is: 10.5 to 13.5 kilopascal (kPa)

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Oxygen

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Oxygen

Pulse oximetry is a test used to measure the oxygen level (oxygen saturation) of the blood. It is an easy, painless measure of how well oxygen is being sent to parts of your body furthest from your heart, such as the arms and legs.

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Oxygen

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Oxygen

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Oxygen

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Warfarin

Name : Warfarin / Warfarin sodium

Drug class:
Anticoagulant (Vitamin K antagonist) aka as blood thinners

Indication:
Prophylaxis (treatment given to prevent disease)

venous thromboembolism

pulmonary embolism

thromboembolism with atrial fibrillation

thromboembolism with cardiac valve replacement

thromboembolic events post myocardial infarction.

Mechanism of action:
Warfarin is a [vitamin K] antagonist which acts to inhibit the production of vitamin K by vitamin K epoxide reductase.

Contraindications:
Postpartum (delay warfarin until risk of haemorrhage (blood loss) is low—usually 5–7 days after delivery)

conditions in which risk of bleeding is increased

history of gastrointestinal bleeding

Side effects:

Haemorrhage, nausea, vomiting, diarrhoea, jaundice, hepatic dysfunction, pancreatitis.

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Warfarin

The INR, or international normalised ratio, can also be used to check if you have a blood clotting problem
In healthy people an INR of 1.1 or below is considered normal. An INR range of 2.0 to 3.0 is generally an effective therapeutic range for people taking warfarin for certain disorders.
warfarin should be stopped about 5 days before surgery

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Warfarin

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Warfarin

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Warfarin

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Apixaban

Class: Anticoagulant (factor Xa inhibitors)

Indication:
Reduces the risk of stroke and systemic embolism in nonvalvular atrial fibrillation

Prophylaxis of deep vein thrombosis leading to pulmonary embolism in patients after knee or hip surgery.

Mechanism of action:
Selectively inhibits factor Xa in its free and bound forms, independent of antithrombin III. Apixaban also inhibits prothrombinase. These effects prevent the formation of a thrombus.

Contraindications:
Clinically significant bleeding

Severe hypersensitivity (i.e., anaphylactic reactions)

Side effects:
Anaemia; haemorrhage; nausea; skin reactions

Apixaban

Well’s scoring system
The Well’s score is a useful tool for risk stratifying patients with a suspected PE.

Points are allocated as follows:
-3 points:
Clinical signs and symptoms of a deep vein thrombosis (DVT)
If no alternative diagnosis is more likely than a PE

-1.5 points:
Tachycardia (heart rate >100 beats/minute)
If the patient has been immobile for more than 3 days or has had major surgery within the last month
If the patient has had a previous PE or DVT

-1 point:
If the patient presents with haemoptysis
If there is an active malignancy

If the Well’s score is 4 or less the D-dimer should be measured

Salbutamol

Class: beta-2 adrenergic receptor agonist (bronchodilator)

Indication:
Asthma, COPD & other conditions with reversible airways obstruction Prophylaxis of allergen or exercise-induced bronchospasm

Mechanism of action:
Salbutamol acts on beta-2 adrenergic receptors to relax the bronchial smooth muscle. It also inhibits the release of immediate hypersensitivity mediators from cells, especially mast cells

Contraindications:
Arrhythmias,

cardiovascular disease; diabetes (risk of hyperglycaemia and ketoacidosis, especially with intravenous use)

Hypertension

hyperthyroidism; hypokalaemia; susceptibility to QT-interval prolongation

Side effects:

Arrhythmias; headache; palpitations; tremor

Salbutamol

Nicotine

Drug Class:

Indication:
Nicotine replacement therapy in individuals who smoke less than 20 a day.

Taken by mouth: chewing gum, tablet, inhalator, lozenges

Transdermal application: using patches

Mechanism of action:
Nicotine is a stimulant drug that acts as an agonist at nicotinic acetylcholine receptors.

Contraindications:
Diabetes mellitus, Gastrointestinal disease, Severe renal impairment, Uncontrolled hyperthyroidism, History of epilepsy.

Side effects:
Dizziness; headache; hyperhidrosis; nausea; palpitations; skin reactions; vomiting

Noradrenaline

Class: catecholamine family / neurohormone

Binds to alpha1 (alpha-1), alpha-2, and beta receptors

Indication:
Epinephrine injection is indicated in the emergency treatment of type I allergic reactions, including anaphylaxis.

Acute hypotension

Mechanism of action:

Epinephrine acts on alpha and beta-adrenergic receptors

Contraindications:
Hypertension

Side effects:
- Acute glaucoma, anxiety, cardiomyopathy, high blood pressure

Blood pressure

Normal blood pressure is 120/80mmHg
so a systolic pressure under 120
and a diastolic blood pressure under 80
having a systolic value between 120-139
and diastolic value between 80-89
this is known as being prehypertension
systolic bp of 140 ( and above)
diastolic bp of 90 (and above)
this is recognised as hypertension
Blood pressure = CO x SVR

When blood vessels restricts it results in increased SVR which increases BP

Increasing:
Cardiac output
stroke volume
heart rate
systemic vascular resistance
contractility
blood volume will all increase blood pressure
If we reduce any of teh above we will decrease blood pressure
reduce SVR: by dilating blood vessels
reduce heart rate
reduce muscle contractility ( calcium causes muscles to contract by reducing calcium there will be less contraction)
reduce blood volume ( inhibiting renin angiotensin system or by giving patient a diuretic)

There is 3 types of hypertension

Primary hypertension: we don’t know the cause
Secondary hypertension: normally due to some other underlying condition
Malignant hypertension: rapid onset of hypertension which is associated with organ failure

What are ACE inhibitors used for ?

are used for the treatment of high blood pressure and heart failure.
They work by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart

Selective Beta blockers

At all sympathetic neurons targeting an organ we always release adrenaline or noradrenaline
Adrenaline binds to specific receptors: a1, a2, B1, B2 and B3 receptors
the receptors located specifically on the heart are B1 receptors
Which means for beta blockers you can have selective B1 blockers such as atenolol.
when the sympathetic neurons release adrenaline neurotransmitter where they bind to b1 receptors on the heart it causes:
increased heart rate
increased contractility
with a better blocker
heart does not get stimulated reducing heart rate and contractility

What are ACE inhibitors ?

before AT1 (angiotensin 1) is converted to AT2 (angiotensin 2) we need the enzyme ACE (angiotensin converting enzyme to do that)

Angiotensin 2 causes:
- vasoconstriction
- also results in the release of aldosterone. Aldosterone promotes sodium reabsorption back into the kidneys and back into the blood. The more sodium in the blood, the more water that comes into the blood which increases blood volume, therefore blood pressure.
- stimulates the release of ADH (antidiuretic hormone). ADH tells the kidneys to hold onto water, which increases blood volume therefore increases blood pressure.

Therefore AT2 is released into the blood to increase blood volume and blood pressure.
And if we inhibit AT2 production by ACE inhibitors you reduce blood pressure.
Common ACE inhibitor is ENALAPRIL

What are Angiotensin 2 receptor antagonists ?

Angiotensin 2 receptor antagonists stop angiotensin 2 from binding to its receptors and causing all of its pressure increasing effects.

Example: Candesartan

What are calcium (Ca2+) channel blockers ?

Calcium is one of the most abundant extracellular cations. Its positively charged and located outside of the cell.

When calcium enters the cell it can:
- act as a secondary messenger, so it can tell certain things to happen inside the cell
- or it can tell muscles to contract.

if you block calcium from entering myocardium heart muscle cells you can reduce its ability to contract.
certain cells of the heart SAN and AVN in order for them to depolarize they require calcium to come in which means these calcium channel blockers can inhibit or reduce the depolarization of the nodal cells.
This slows the contraction rate and therefore the heart rate.

There are 3 different types of calcium channel blocker drugs?

There is not one type of calcium channel there are many different types and they are located in different parts of teh body. One organ may have many different types of calcium channels.

The different types of calcium channels have certain specificity and will have different effects.

Nifedipine
Veramapil
Diltiazem

Nifedipine acts at calcium channels at vascular smooth muscle. This blocks calcium’s effect, reducing vasoconstriction resulting in vasodilation, which reduces (SVR) systemic vascular resistance which reduces blood pressure.
It also has an effect as an aldosterone receptor antagonist. If you stop aldosterone from having an effect you stop sodium reabsorption which stops water reabsorption, which reduces blood volume and blood pressure

Verapamil:

-blocks calcium channels at the nodes, SA node and AV node (nodes) and conductive tissue. This helps reduce arrhythmias.

Diltiazem:

has its effects at the coronary vasculature

Diuretics

Diuretics act at the kidneys specifically at the nephrons and cause sodium reabsorption. Which means increasing the amount of sodium that gets peed out, which increases teh amount of water that follows which increases the volume that you pee out. This reduces blood volume and blood pressure.
The most common type of diuretics are the thiazides.
The thiazides work at the (DCT) distal convoluted tubule
Why would not use a loop diuretic acting at the loop of henle. They are potent and short lasting.
Whereas thiazides are longer lasting and tend to be more effective as antihypertensive medications. They are commonly used in conjunction with another antihypertensive drugs

How do thiazides work:

at the DCT they stop sodium from being reabsorbed back into the body. This means sodium stays in the DCT so water stays in the DCT. So water gets peed out which reduces blood volume therefore blood pressure.
These sort of diuretics also flush potassium out of your body so you need to be careful measuring your potassium levels when a patient takes this medication . I’m

Anti-hypertension drugs

-Betablockers are the lols : propanolol

ACE inhibitors are the prils: Enalapril
Angiotensin 2 antagonists are the sartans: Candesartan
calcium channel blockers

Dobutamine

Class: Beta-1- agonist (cardiac stimulant)

Indication: Patients who require positive inotropic support in the treatment of cardiac decompensation due to depressed contractility resulting either from organic heart disease or from cardiac surgical procedures

Mechanism of action: -stimulates beta-1 receptors of the heart to increase contractility and stroke volume, resulting in increased cardiac output.

Contraindications:
Phaeochromocytoma (tumour on adrenal glands)

Side effects: Chest pain, palpitations, headaches, tremors, shortness of breath, nausea, and vomiting

Isoprenaline

Class: catecholamine non-selective beta-agonist

Indication:
- Bradycardia especially in postoperative cardiac patients
- heart block

Cardiac Arrest

Heart Block

Adam-Stokes Attacks

Mechanism of action:

-Agonism of beta-1 and beta-2 adrenergic receptors.

Agonism of beta-1 adrenergic receptors lead to increased strength of contractility, conduction of nerve impulses, speed of relaxation, and rate in the heart
Agonism of beta-2 adrenergic receptors leads to glycogenolysis in the liver

Contraindications:
- Tachyarrhythmias

Tachycardia

Heart block caused by digitalis intoxication

Side effects:

Dyspnoea, angina, palpitations, pulmonary Edema, flushing of the skin

Atenolol

Class: selective β-1 receptor antagonist

Indication: Hypertension, angina, cardiac arrhythmias, heart failure and glaucoma.

Mechanism of action:
Selective to Beta 1 adrenoceptors, Atenolol acts as an antagonist. It does not pass the blood-brain barrier, resulting in no CNS side effects.

Contraindications:
Asthma, uncontrolled heart failure, hypotension, metabolic acidosis.

Side effects:
Abdominal discomfort, bradycardia, peripheral coldness, dyspnoea, gou

Propranolol

Class: non selective competitive β-receptor antagonist

Indication: Hypertension angina, cardiac arrhythmias, infantile haemangioma, tetralogy of Fallot, hyperthyroidism.

Mechanism of action: Blocks Beta 1 and 2 adrenoceptors equally.

Contraindications: Asthma, uncontrolled heart failure, hypotension, metabolic acidosis

Side effects: Abdominal discomfort, bradycardia, peripheral coldness dyspnoea, gout

Bendroflumethiazide

Class: Thiazide type diuretic which inhibits the sodium chloride cotransporter

Indication: Hypertension, angina, cardiac arrhythmias, infantile haemangioma, tetralogy of Fallot, hyperthyroidism.

Mechanism of action:
-Thiazides act by inhibiting NaCl reabsorption by binding to the symporter responsible for electroneutral cotransport of Sodium and Chloride ions.
- Thiazides stop sodium from being reabsorbed into the body, they keep sodium in the kidneys, which causes more water to enter the kidneys and be excreted as urine.
-Therefore, excretion of Sodium and chloride increases, along with accompanying water.

Contraindications:
Addison’s disease; hypercalcaemia, hyponatraemia; refractory hypokalaemia, symptomatic hyperuricaemia

Side effects:
Mild gastro-intestinal disturbances, postural hypotension, impotence, altered plasma-lipid concentration, gout.

Amiodarone

Class: Potassium channel blocker

Indication: Tachycardia associated with Wolff-Parkinson-White syndrome. Supraventricular and ventricular tachyarrhythmias.

Mechanism:
Act by slowing repolarisation and prolonging action potential and refractory period in all cardiac tissues. Amiodarone has blocking actions on several channels (potassium ion and inactivated sodium ion channels) and beta adrenoceptors.

Contraindication:
Sinus bradycardia, sinoatrial heart block, thyroid dysfunction, severe arterial hypotension.

Side effects:
Nausea, vomiting, taste disturbances, photosensitive skin rashes, bluish discolouration of the skin, thyroid abnormalities, pulmonary fibrosis, neurological and gastro-intestinal disturbances.

Ramipril

Class: ACE (angiotensin-converting enzyme) inhibitor

Indication: Hypertension, prevention of heart failure progression, post-myocardial infarction & heart Failure with reduced ejection fraction

Mechanism: Ramipril inhibits angiotensin-converting enzyme and decreases angiotensin II formation. As a result, sympathetic activity goes down, sodium and water reabsorption from the kidneys reduces, smooth muscles in the arterioles also relax. As a result, blood pressure decreases and increases the supply of blood and oxygen to the heart.

Contraindication:
Hypersensitivity, angioedema, hyperkalemia (high K), Hyponatremia (low Na) & Pregnancy

Side effects:
Dry cough, Postural hypotension (low blood pressure when standing after sitting or lying down), anxiety, Angioedema

Amlodipine

Class: Calcium channel blockers

Indication: To treat high blood pressure in adults and children 6 years and older. It is also used to treat certain types of anginas (chest pain) and coronary artery disease (narrowing of the blood vessels that supply blood to the heart).

Mechanism:
Decreases blood pressure by inducing smooth muscle relaxation and vasodilatation.

Amlodipine works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Reduced intracellular calcium leads to decreased vascular smooth muscle contractility, increased smooth muscle relaxation, and resultant vasodilation.

Contraindication: Known hypersensitivity, severe aortic stenosis, unstable angina, severe hypotension, heart failure, and hepatic impairment

Side effects: Peripheral oedema, dizziness, flushing, among others.

Doxazosin

Class: Competitive Alpha1-antagonist

Indication:Prostate gland enlargement, Hypertension

Mechanism: Doxazosin competitively inhibits post-synaptic alpha1-adrenergic receptors causing vasodilation of arterioles and veins, which results in decreased total peripheral resistance and blood pressure.

Contraindication: Hypersensitivity to doxazosin or other quinazolines & Pregnancy

Side effects:
Feeling weak, sleepy or dizzy, Headaches, Swollen feet, ankles or fingers, Urinary tract infection (UTI) or cystitis, Stomach pain or back pain, Feeling sick (nausea), indigestion or heartburn.

Opiate question

What are ACE inhibitors used for ?

are used for the treatment of high blood pressure and heart failure.
They work by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart

What are calcium (Ca2+) channel blockers ?

Calcium is one of the most abundant extracellular cations. Its positively charged and located outside of the cell.

When calcium enters the cell it can:
- act as a secondary messenger, so it can tell certain things to happen inside the cell
- or it can tell muscles to contract.

if you block calcium from entering myocardium heart muscle cells you can reduce its ability to contract.
certain cells of the heart SAN and AVN in order for them to depolarize they require calcium to come in which means these calcium channel blockers can inhibit or reduce the depolarization of the nodal cells.
This slows the contraction rate and therefore the heart rate.

Atropine

Digoxin

Sympathetic nervous system is part of the autonomic nervous system

Sympathetic nervous system is what is activated during our fight and flight response
Adrenal glands also release adrenaline
The neurotransmitter used to communicate between sympathertic nerves is noradrenaline (norepinephrine) or adrenaline ( epinephrine)
All of these neurotransmitters bind to adrenergic receptors.
There are a number of adrenergic receptors a1, a2, b1, b2, and b3.

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Block 2 drugs Flashcards

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