pharmacology full syllabus.

 

Ques:- what do you mean by biotransformation or metabolism of drugs. discuss different types of biotransformation?

Biotransformation of drugs is like changing the shape and nature of medicines in our body so they can be handled and removed easily.

There are two main steps in this process:

Step 1 - Phase I Reactions: Altering the Drug

1. Oxidation: Enzymes in our body add oxygen to the medicine, making it a bit different. This might add things like hydroxyl groups to the medicine.
2. Reduction: Enzymes add electrons to the medicine, making it simpler and changing its properties.
3. Hydrolysis: Water is used to break apart the medicine into smaller pieces, making it easier to manage.

Step 2 - Phase II Reactions: Adding Water-Soluble Tags

1. Glucuronidation: Our body sticks a special tag called glucuronic acid onto the medicine. This tag helps the medicine dissolve in water, so our body can remove it through urine.
2. Sulfation: Another tag, sulfate, is attached to the medicine. This tag helps the medicine to easily dissolve in water for elimination.
3. Amino Acid combining: Amino acid combines with medicine, which makes it more water-friendly and simpler to eliminate.
4. Glutathione Combining: Glutathione combines with medicines which makes it risky and  easier to eliminate from the body.

In summary, biotransformation is like giving medicines a makeover in two steps. First, they're changed to make them simpler or different. Then, special tags are added to help them dissolve in water, so the body can easily get rid of them through urine or other ways. This process ensures medicines are safely used and removed from our bodies.

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Ques- Describe briefly about anti cholinesterase drugs?

Anti-cholinesterase drugs are medicines that block the activity of an enzyme called "cholinesterase." This enzyme breaks down a neurotransmitter called "acetylcholine" which helps nerve signals to work properly. By blocking the enzyme, these drugs increase the amount of acetylcholine in the brain, which can improve nerve communication and help with conditions like Alzheimer's disease and certain nerve-related problems.

Reversable and irreversible choline esterase inhibitors

Reversible Cholinesterase Inhibitors: Reversible cholinesterase inhibitors are drugs that temporarily slow down the enzyme responsible for breaking down acetylcholine (a crucial neurotransmitter) in the brain. This delay enhances the effects of acetylcholine, a crucial neurotransmitter, by extending its presence in the brain. It's akin to creating a momentary obstacle for the enzyme, promoting better communication between nerve cells. These inhibitors are utilized to address conditions like Alzheimer's disease, where nerve cell communication is impaired.

Example -

Irreversible Cholinesterase Inhibitors: Irreversible cholinesterase inhibitors are medications that form strong and permanent connections with the enzyme that breaks down acetylcholine. Once attached, the enzyme's function is permanently halted. This is comparable to locking a door without the possibility of unlocking it. While these inhibitors offer a more potent and sustained impact on nerve communication, they require cautious consideration due to their irreversible nature.

Example -

 

Define pharmacological classification and examples of anticholinergic drugs?

Anticholinergic drugs are a type of medication that blocks the effects of acetylcholine (a neurotransmitter)

Acetylcholine helps nerve cells communicate with each other and control various activities like muscle movement, digestion, and more.

These drugs work by inhibiting the action of acetylcholine in the nervous system.

Anticholinergic drugs serve as regulators or modifier of the messages between nerve cells. By blocking the effects of acetylcholine, these drugs can impact various bodily functions.

They are used for various purposes, including reducing muscle spasms, treating certain gastrointestinal conditions, and managing symptoms like excessive sweating or overactive bladder.Top of Form

Classification of Anticholinergic Drugs:

1] Muscarinic Antagonists.

2] Nicotinic Antagonists.

 

1] Muscarinic Antagonists: These drugs block the action of acetylcholine at muscarinic receptors, which are found in various organs like the heart, smooth muscles, and glands.

This category of drugs is used for a variety of purposes, including treating conditions such as overactive bladder, motion sickness, gastrointestinal disorders, and certain respiratory issues.

Examples-

Atropine: Often used to dilate (widen) the pupils during eye exams and surgeries, and to decrease saliva production.

Hyoscine: Used to alleviate motion sickness, nausea, and vomiting.

Tiotropium: An inhaled medication for chronic obstructive pulmonary disease (COPD) and asthma.

Oxybutynin: Prescribed to manage overactive bladder.

Cyclopentolate: Used to dilate the pupil and temporarily paralyze the eye's focusing muscles for eye examinations.

 

2] Nicotinic Antagonists: Nicotinic antagonists are drugs that impact the communication between nerves and muscles.

They can change the way nerves send messages to muscles, which can affect muscle activity and responsiveness.

This interference can lead to muscle relaxation and decreased muscle activity.

Example-

Gallamine: Used as a muscle relaxant during surgery.

Atracurium: Another muscle relaxant for surgical procedures requiring muscle relaxation.

Cisatracurium: A neuromuscular blocking agent used in anaesthesia.

Mivacurium: A short-acting muscle relaxant used during anaesthesia.

Rocuronium: A non-depolarizing muscle relaxant for surgical procedures.

Hexamethonium: Formerly used to lower blood pressure by blocking certain nerve signals.

 

Define Anti glaucoma drugs and classify it / what are the drugs used in glaucoma?

Glaucoma: Glaucoma is a group of eye conditions that can lead to damage to the optic nerve and can result in blindness. It's often associated with increased pressure within the eye.

The optic nerve is responsible for transmitting visual information from the eye to the brain. In glaucoma, the optic nerve becomes damaged, which can result in blindness.

 

Anti Glaucoma drugs -
Anti-glaucoma drugs are medications used to treat glaucoma -- a condition that affects the eyes and can lead to vision loss.

These drugs work by reducing the pressure inside the eyes [intraocular pressure] Lowering this pressure helps to prevent damage to the optic nerve and preserve vision.

There are several classes of anti-glaucoma drugs, each with different mechanisms of action. These drugs can be used alone or in combination to effectively manage intraocular pressure.

Here are some common classes of anti-glaucoma drugs:

Beta-Blockers: These drugs reduce the production of aqueous humor -- the fluid that fills the front part of the eye. This decreases intraocular pressure.

They are available in eye drop form. Examples include timolol and betaxolol.

Prostaglandin Analogues: These drugs increase the drainage of fluid from the eye, which helps to lower intraocular pressure.

They are often used as first-line treatment due to their effectiveness and once-a-day dosing.

Examples include latanoprost, bimatoprost, and travoprost.

Alpha Agonists: These drugs both decrease fluid production and increase fluid drainage from the eye, leading to lowered pressure.

They are available as eye drops. Examples include brimonidine and apraclonidine.

Carbonic Anhydrase Inhibitors: These drugs reduce the production of aqueous humor, thus lowering intraocular pressure.

They can be used as eye drops or taken orally. Examples include dorzolamide (eye drop) and acetazolamide (oral).

Combination Drugs: In some cases, doctors may prescribe eye drops that contain a combination of different anti-glaucoma medications to target multiple aspects of intraocular pressure regulation.

Cholinergic agents: Cholinergic agents can acts as a anti-glaucoma drugs that boost fluid drainage from the eye by activating certain receptors.

This reduces intraocular pressure, a key factor in glaucoma. While historically used, they're now less common due to newer options. Side effects can include blurred vision and pupil constriction. They're typically considered when other treatments aren't suitable.

Examples- Pilocarpine and carbachol.

 

Define anticoagulants. Give its type. describe pharmacological actions, dose.

Anticoagulants are medications that help prevent the formation of blood clots or reduce the risk of existing blood clots from becoming larger.

They are given to people at a high risk of getting clots, to reduce chances of developing serious conditions such as stroke and heart attack.

They are commonly used to treat and prevent conditions such as deep vein thrombosis (DVT), pulmonary embolism (PE), atrial fibrillation, and certain heart valve disorders.

Anticoagulants work by interfering with the blood clotting process, thus reducing the likelihood of dangerous clots forming in blood vessels.

 

Pharmacological Actions: Anticoagulants slow down the clotting process by inhibiting specific clotting factors or proteins that promote clot formation. This reduces the risk of abnormal clot formation within blood vessels, which can lead to serious complications like strokes or heart attacks.

Dosing: Dosages for anticoagulants vary - based on age, weight, sex, health, other medical conditions. Proper dosing is crucial to prevent clots.

 

Contraindications: Anticoagulants should be used with caution in situations involving active bleeding, bleeding disorders, surgeries, stroke etc. Medical guidance is crucial to ensure safe and appropriate use.

 

Types of Anticoagulants:

1. Heparins: This is mainly given by injections (e.g., enoxaparin) and is often used in hospitals for acute situations.
2. Vitamin K Antagonists (VKA) -  are a class of anticoagulant medications that work by interfering with the body's ability to utilize vitamin K for the production of blood clotting factors.

Vitamin K is a vital nutrient that helps in the synthesis of these clotting factors.

Example- warfarin [most commonly prescribed anticoagulant]

MOA of warfarin –

3. Warfarin is an anticoagulant that works by interfering with the body's ability to utilize vitamin K to produce blood clotting factors.

Vitamin K is essential to produce certain clotting factors in the blood. This leads to a decrease in the production of clotting.

As a result, blood's ability to form clots is weakened, which helps prevent abnormal and harmful blood clots.

Regular monitoring and adjustment of warfarin dosage are needed to balance its benefits in preventing clots with the risk of bleeding.

4. Direct Oral Anticoagulants (DOACs): represent a more recent class of anticoagulant medications.

These medications are designed to prevent abnormal blood clotting in a more targeted and efficient manner than traditional Vitamin K Antagonists (VKAs).

Unlike VKAs, DOACs directly target specific components of the blood clotting cascade.

MOA of these drugs –

• Rivaroxaban and Apixaban: These drugs are known as Factor Xa inhibitors. Factor Xa is a critical protein involved in the formation of blood clots. By inhibiting Factor Xa, these medications prevent the formation of thrombin. Without thrombin, blood clots are less likely to develop.
• Dabigatran: This medication is a direct thrombin inhibitor. Thrombin is an enzyme that plays a central role in the clotting process by converting fibrinogen into fibrin.

By inhibiting thrombin, dabigatran helps prevent the formation of fibrin and subsequent clot development.

• Edoxaban: Similar to rivaroxaban and apixaban, edoxaban is another Factor Xa inhibitor that interferes with the clotting process by targeting Factor Xa and inhibiting its ability to generate thrombin.

 

 

QUES: What do you understand by bronchodilator? Describe its classification.

A bronchodilator is a medication used to relax and widen the airways in the respiratory system.

By opening the airways, bronchodilators improve the airflow and make it easier for individuals to breathe.

And hence helps to alleviate the symptoms of respiratory conditions such as asthma, chronic obstructive pulmonary disease (COPD), and bronchitis.

Bronchodilators can be classified into several categories based on their mechanisms of action:

1. Beta-2 Agonists: Also known as beta aerogenic bronchodilators.  

Dilates the bronchial airways by relaxing the muscles that surrounds the airways.

These medicines stimulate beta 2 receptors on the smooth muscle cells causing these cells to relax.

These are of two types.

• Short-acting beta-2 agonists (SABAs): These drugs provide rapid relief of bronchospasm and are often used as rescue inhalers during acute asthma attacks. Examples include albuterol and levalbuterol.
• Long-acting beta-2 agonists (LABAs): These bronchodilators have a longer duration of action and are typically used for maintenance therapy in conditions like COPD. Examples include salmeterol and formoterol.
1. Anticholinergics:

Blocks the effects of acetylcholine [a neurotransmitter used by the brains to transmit signal to muscles] on airways and nasal passages.

The cholinergic nerves going to the lungs cause narrowing of airways. The anticholinergic action blocks the effects of cholinergic nerves and hence dilates the airways.

• Short-acting anticholinergics (SAMA): These drugs block the action of acetylcholine, a neurotransmitter that causes airway constriction. Ipratropium bromide is a common SAMA used to relieve bronchospasm.
• Long-acting anticholinergics (LAMA): These bronchodilators have a sustained effect and are used for long-term management of conditions like COPD. Tiotropium is a well-known LAMA.
2. Combination Bronchodilators:
• Some medications combine different classes of bronchodilators to provide a more comprehensive approach to managing respiratory conditions. For example, a combination of a LABA and an inhaled corticosteroid is often used in the treatment of moderate to severe asthma.

It's important to note that while bronchodilators can provide rapid relief of symptoms, they do not address the underlying conditions. Therefore, they are often used in combination with anti-inflammatory medications like corticosteroids to manage the respiratory conditions effectively.

Bronchodilators are typically administered via inhalation using devices such as metered-dose inhalers (MDIs), dry powder inhalers (DPIs), or nebulizers.

The choice of bronchodilator and inhalation device depends on the specific condition, the severity of symptoms, and individual patient factors.

 

What do you understand by expectorant. Classify?

 

An expectorant is a medication that people can use when they have a cough that produces thick mucus that often accompanied with cold, bronchitis, or infections.

The main job of an expectorant is to make this mucus thinner, which in turn makes it easier for you to cough it and clear out your airways.

Classification of expectorant:

Learn from page number 77 – book pharmacology – orange colour.

 

Give informative note on antitussive and briefly discuss about it.         Chapter 7

An antitussive is a type of medication that relieves coughing.

Coughing is a natural reflex that helps clear the airways or mucus. However, excessive coughing can be harmful, leading to sore throat, chest discomfort, and sleep disturbances. Antitussives are used to mitigate these symptoms by reducing the urge to cough.

There are two primary categories of antitussives:

1. Opioid Antitussives: These are antitussive medications that contain opioids like codeine or hydrocodone.

Opioid antitussives act on the central nervous system to suppress the cough reflex.

They are typically prescribed for severe coughing that does not respond to other treatments.

 However, due to their potential for side effects and the risk of dependence, they are used cautiously and for short durations.

Patients using opioid antitussives should use them strictly as directed by a healthcare professional. These medications should be reserved for cases where the benefits outweigh the risks, and they should not be used for a prolonged period.

2. Non-Opioid (Non-Narcotic) Antitussives: Non-opioid antitussives are a safer and more commonly used.

They work by directly acting on the cough reflex in the brain or the nerve endings in the throat to reduce the urge to cough.

Dextromethorphan is a widely used non-opioid antitussive found in many over-the-counter cough syrups and medications.

Non-opioid antitussives are generally considered safer than opioid counterparts and are suitable for managing most common coughs associated with conditions like colds, allergies, or irritants.

It's important to note that while antitussives can provide relief from coughing, they do not address the underlying cause of the cough. Therefore, antitussives are generally recommended for short-term use to alleviate discomfort while allowing the body to heal.

Antitussives are available in various forms, including liquid syrups, tablets, and capsules.

When using antitussive medications, it's crucial to follow the recommended dosage instructions provided on the label or as directed by a healthcare professional to ensure safe and effective use.

 

Chapter 8

What are antiemetic drugs? Classify it.

antiemetic drugs are medications used to prevent or relieve nausea and vomiting. These two symptoms are very common and can be caused by many different conditions like during medication or during therapies.

Though vomiting is considered to be a protective reflex of the body to expel the toxic substance out. But antiemetic drugs are often necessary to suppress vomiting especially if there’s severe dehydration.

They are classified into several categories based on their mechanisms of action and also on specific types of nausea and vomiting.

Here are some common classes of antiemetic drugs:

Dopamine Receptor Antagonists: These drugs work by blocking dopamine receptors in the brain. They are mainly used to prevent nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. Examples include metoclopramide and prochlorperazine.

Cannabinoids: Medications containing synthetic cannabinoids are prescribed to alleviate nausea and vomiting, often in cancer patients undergoing chemotherapy or individuals with specific medical conditions. These drugs exert their effects by interacting with the endocannabinoid system in the body.

Ex- dronabinol and nabilone

Anticholinergics: anticholinergic drug, is available as a transdermal patch [kaan k peche tikiya si laga di jati h] and is used to prevent motion sickness and associated nausea.

Ex- Scopolamine

Benzodiazepines: Occasionally, benzodiazepines [like lorazepam and diazepam] may be employed to control nausea and vomiting associated with anxiety or specific medical conditions. Their anxiolytic properties can help alleviate symptoms indirectly.

 

Antihistamines: Certain antihistamines  [such as dimenhydrinate and meclizine] are effective in preventing motion sickness and alleviating nausea related to vestibular disturbances.

 

Serotonin (5-HT3) Receptor Antagonists: One major class of antiemetics includes 5-HT3 receptor antagonists, such as ondansetron, granisetron, and palonosetron.

These drugs operate by blocking serotonin receptors in both the gastrointestinal tract and the brain, effectively interrupting the signal that triggers nausea and vomiting. They are widely employed in preventing and managing nausea and vomiting induced by chemotherapy and postoperative procedures.

 

Define laxatives and discuss its type?

Laxatives are the substances that are used to promote bowel movements and relieve constipation.

They are commonly employed when individuals experience constipation, which can be caused by various factors such as dietary changes, medication side effects, or underlying medical conditions.

Laxatives work by softening the stool, increasing stool volume, or promoting bowel movement.

Here are some common types of laxatives along with examples:

1. Bulk-Forming Laxatives:

Definition: Bulk-forming laxatives are substances that add bulk and moisture to the stool, making it softer and easier to pass.

They work by increasing the volume of stool and promoting regular bowel movements.

• Examples: Psyllium (Metamucil), methylcellulose (Citrucel), and wheat dextrin (Benefiber).
1. Osmotic Laxatives:

Definition: Osmotic laxatives are substances that draw water into the intestines, softening the stool and increasing bowel movements.

They work by creating an osmotic gradient in the intestines, encouraging water retention in the stool.

• In short: Osmotic laxatives draw water into the intestines, softening the stool and increasing bowel movements.
• Examples: Magnesium hydroxide (Milk of Magnesia), magnesium citrate, lactulose, and polyethylene glycol (PEG).
2. Stimulant Laxatives:
• Mechanism: Stimulant laxatives work by irritating the intestinal lining, leading to increased muscular contractions in the intestines and promoting bowel movements.
• They work by stimulating the muscles of the intestines.
• Examples: Senna (Senokot), bisacodyl (Dulcolax), and castor oil.
3. Emollient or Stool Softeners:

Definition: Emollient or stool softeners are laxatives that help soften the stool by adding moisture to it, making it easier to pass.

They work by allowing the stool to absorb more water.

• Examples: Docusate sodium (Colace), docusate calcium (Surfak).
4. Lubricant Laxatives:

Definition: Lubricant laxatives are medications that coat both the stool and the intestinal walls, allowing for smoother passage of feces. They work by reducing friction between the stool and the intestinal walls.

• Examples: Mineral oil (often used sparingly due to concerns about aspiration into the lungs).
5. Saline Laxatives:

Definition: Saline laxatives contain magnesium or other salts that draw water into the intestines, softening the stool and promoting bowel movements. They work by creating an osmotic effect in the intestines.

• Examples: Magnesium sulfate (Epsom salt), magnesium citrate.
6. Prokinetic Agents:
• Mechanism: These medications increase the motility of the intestines, facilitating the movement of stool through the digestive tract.
• They work by promoting coordinated contractions of the intestinal muscles.
• Examples: Prucalopride (Resolor), lubiprostone (Amitiza).

It's important to note that laxatives should be used cautiously and under the guidance of a healthcare professional.

Overuse of laxatives can lead to dependence, electrolyte imbalances, dehydration, and other health issues.

Laxatives should not be used as a long-term solution for constipation.

Additionally, the choice of laxative depends on factors such as the severity of constipation, the individual's overall health, and any underlying medical conditions or medications they may be taking.

Consulting with a healthcare provider is essential to determine the most appropriate type of laxative and dosage for a specific situation.

Top of Form

 

Define Purgatives. Classify it with examples.

Purgatives are a category of strong laxatives that are specifically designed to induce rapid and extensive bowel movements. They are typically used for more aggressive or therapeutic purposes, such as clearing the intestines before certain medical procedures or surgeries, rather than for routine relief of constipation. Purgatives are known for their potent and often drastic effects on bowel movements.

Purgatives can be classified into several subcategories based on their mechanisms of action and specific uses. Here are some common types of purgatives along with examples:

1. Osmotic Purgatives:
• Definition: Osmotic purgatives are substances or medications that create an osmotic effect in the intestines, drawing water into the bowel and leading to rapid, watery bowel movements. They are used to evacuate the bowel before medical procedures or surgeries.
• Examples: Sodium phosphate (Fleet Phospho-Soda), sodium picosulfate (Prepopik), and magnesium citrate.
2. Saline Purgatives:
• Definition: Saline purgatives contain magnesium or other salts that induce a powerful osmotic effect in the intestines, leading to the evacuation of stool. They are used for bowel cleansing prior to medical examinations or surgery.
• Examples: Magnesium sulfate (Epsom salt) and sodium sulfate.
3. Stimulant Purgatives:
• Definition: Stimulant purgatives are medications that strongly irritate the intestinal lining, causing intense contractions of the intestinal muscles and rapid bowel movements. They are used for colon cleansing and before certain medical procedures.
• Examples: Bisacodyl (Dulcolax) and castor oil.
4. Polyethylene Glycol (PEG) Purgatives:
• Definition: PEG purgatives are high-molecular-weight compounds that work by causing an osmotic effect in the intestines. They are used for bowel cleansing in preparation for colonoscopy and other medical procedures.
• Examples: Polyethylene glycol-electrolyte solutions (e.g., GoLYTELY, Miralax).
5. Sorbitol Purgatives:
• Definition: Sorbitol is a sugar alcohol that acts as an osmotic purgative, drawing water into the intestines and promoting bowel evacuation. It is used in some bowel preparation solutions.
• Examples: Sorbitol-containing bowel preparations.
6. Castor Oil Purgatives:
• Definition: Castor oil is a natural purgative that works by irritating the intestinal mucosa and stimulating strong bowel contractions. It has been used historically for its laxative effects.
• Examples: Castor oil.

It's important to note that purgatives are typically reserved for specific medical indications or surgical procedures, under the guidance of healthcare professionals.

Due to their potent and rapid effects, they are not typically used for routine constipation relief, as milder laxatives are more suitable for such purposes.

Overuse or misuse of purgatives can lead to electrolyte imbalances, dehydration, and other health complications. Therefore, they should only be used as directed by a healthcare provider…

 

Define antidiarrheal drugs. Classify it.

 

Antidiarrheal drugs are a category of medications used to manage diarrhoea, a common gastrointestinal condition characterized by frequent watery bowel movements.

These drugs work by various mechanisms to slow down or stop the excessive bowel movements and reduce fluid loss associated with diarrhea.

Antidiarrheal drugs can be classified into several categories based on their mechanisms of action and specific applications.

Here are some common classes of antidiarrheal drugs along with examples:

1. Opioid Agonists:
• Mechanism: Opioid agonists work by slowing down bowel motility and reducing the contractions of the intestines, which can help alleviate diarrhea.
• Examples: Loperamide (Imodium) and diphenoxylate/atropine (Lomotil).
2. Bulk-Forming Agents:
• Mechanism: Bulk-forming agents work by absorbing excess water in the intestines, thereby increasing the bulk and consistency of stool. They can help in cases of mild diarrhea.
• Examples: Psyllium (Metamucil) and methylcellulose (Citrucel).
3. Antisecretory Agents:
• Mechanism: Antisecretory agents inhibit the secretion of fluids into the intestines, reducing the volume of diarrhea.
• They are typically used in specific types of diarrhea, such as cholera or traveler's diarrhea.
• Examples: Bismuth subsalicylate (Pepto-Bismol).
4. Adsorbents:
• Mechanism: Adsorbents work by binding to toxins agents in the intestines, preventing them from causing diarrhea. They are primarily used in cases of infectious diarrhea.
• Examples: Kaolin-pectin preparations.
5. Probiotics:
• Mechanism: Probiotics are live beneficial bacteria that can help restore the balance of gut flora, which may be disrupted during diarrhea caused by infections or antibiotics.
• Examples: Lactobacillus acidophilus and Bifidobacterium bifidum.
6. Antimotility Agents:
• Mechanism: Antimotility agents slow down the contractions of the intestines and reduce peristalsis, effectively slowing the passage of stool. They are rarely used due to their potential for dependence and side effects.
• Ex-, such as tincture of opium or paregoric.

It's important to note that while antidiarrheal drugs can provide relief from diarrhea symptoms, they do not address the underlying cause of diarrhea.

Therefore, it's essential to consult with a healthcare professional to determine the cause of diarrhea and to ensure the appropriate treatment.

 

Chapter 09 –

Define diuretics. Classify it?

      A diuretic is a substance that increases the rate of urination by the kidneys, leading to the removal of excess salt (sodium) and water from the body.

 

      Diuretics are commonly used in medical practice to manage conditions such as – hypertension, heart failure, kidney disorders, and edema (fluid retention).

      They help regulate fluid balance and reduce the volume of blood in circulation, which can have therapeutic effects on various health conditions. {specially in hypertension}

      Effect on Blood Pressure {hypertension}: One of the key applications of diuretics is in the management of hypertension (high blood pressure). By reducing the volume of blood circulating through the blood vessels, diuretics can help lower blood pressure, which is important for individuals with hypertension.

      Common Side Effects: Diuretics may cause side effects such as increased urination, dehydration, low blood sodium, and increased thirst. These side effects can vary depending on the type and dosage of the diuretic.

 

 

      Classification -

diuretics can be classified into several categories based on their mode of action and chemical composition.

1. Water Removers: These diuretics help your body get rid of excess water by making you urinate more. Examples include hydrochlorothiazide and chlorthalidone.
2. Loop Cleaners: These diuretics work in the part of your kidneys called the loop of Henle and help remove salt and water.

Examples are furosemide (Lasix) and bumetanide.

3. Potassium Keepers: Some diuretics help your body get rid of extra water but try to keep potassium, an important mineral in your body.

Spironolactone is an example.

4. Sugar Inducers: These diuretics increase the amount of sugar in your urine, which pulls water with it.

Ex - Mannitol is one of these.

5. Acid Blockers: Diuretics like acetazolamide work by blocking a chemical reaction in your kidneys, making you get rid of extra water.

 

1.      Thiazide Diuretics:

·         Example: Hydrochlorothiazide (HCTZ), Chlorthalidone

·         Mode of Action:

·         Thiazide diuretics work on the distal convoluted tubules of the kidneys.

·         They inhibit the sodium-chloride symporter (NCC), which reduces the reabsorption of sodium and chloride ions.

·         This inhibition leads to increased excretion of sodium, chloride, and water in the urine, ultimately reducing fluid volume in the body.

2.      Loop Diuretics:

·         Example: Furosemide (Lasix), Bumetanide

·         Mode of Action:

·         Loop diuretics target the ascending loop of Henle in the kidneys.

·         They inhibit the sodium-potassium-chloride symporter (NKCC2), disrupting the reabsorption of sodium, potassium, and chloride ions.

·         This results in a significant increase in the excretion of sodium and water.

3.      Potassium-Sparing Diuretics:

·         Examples:

·         Aldosterone Receptor Antagonists: Spironolactone, Eplerenone

·         Non-aldosterone Antagonists: Amiloride, Triamterene

·         Mode of Action:

·         Aldosterone Receptor Antagonists: These diuretics block the action of aldosterone, a hormone that regulates sodium and potassium balance in the kidneys. As a result, they reduce sodium reabsorption and promote potassium retention.

·         Non-aldosterone Antagonists: They directly block sodium channels in the renal tubules, reducing sodium reabsorption without significantly affecting potassium levels.

4.      Osmotic Diuretics:

·         Example: Mannitol

·         Mode of Action:

·         Osmotic diuretics increase the osmotic pressure in the renal tubules.

·         This prevents the reabsorption of water, as it creates an osmotic gradient that draws water into the tubules.

·         The outcome is increased urine volume and the excretion of both water and solutes.

5.      Carbonic Anhydrase Inhibitors:

·         Example: Acetazolamide

·         Mode of Action:

·         Carbonic anhydrase inhibitors work in the proximal convoluted tubules.

·         They block the action of the enzyme carbonic anhydrase, which is involved in bicarbonate reabsorption and sodium reabsorption.

·         Inhibition of carbonic anhydrase leads to increased bicarbonate and water excretion.

 

Define antidiuretic. Classify it. Discuss about its pharmacological actions, indications, contraindicators and dose of vasopressin {ADH}.

Definition:
An antidiuretic is something that reduces the production of urine and promote water reabsorption by the kidneys. It helps the body keep more water and produce less urine.

One of the primary antidiuretics used in medicine is vasopressin, also known as antidiuretic hormone (ADH).

 

Classification: Antidiuretics are grouped based on how they work. Vasopressin (ADH) is a natural antidiuretic hormone made by the body.

Synthetic forms of vasopressin can also be used as medications.

Pharmacological Actions: Vasopressin (ADH) does two important things:

1. It helps the kidneys absorb more water, so you make less urine.
2. In higher amounts, it can make blood vessels get narrower, which can lead to increased blood pressure.

Indications: Vasopressin (ADH) is used for:

1. Treating a condition called central diabetes insipidus, where the body makes too much urine due to a lack of ADH {Antidiuretic hormone}.

2.      Sometimes, doctors use it to stop heavy bleeding in the stomach or intestines.

3.      In certain situations, during CPR (when someone's heart stops), vasopressin can help keep blood pressure up.

Contraindications: You should avoid vasopressin if:

1. You're allergic to it.
2. You have severe heart problems because it can make them worse.
3. You have very high blood pressure.

Dose of Vasopressin (ADH):

The amount of vasopressin you get depends on what your doctor thinks is right for you. Always do exactly what your doctor tells you to do with this medicine to make sure you're safe.

 

Define antithyroid drugs. give its type, pharmacological role, clinical roles, clinical use, and side effects.

      Antithyroid drugs are medications used to treat conditions where the thyroid gland produces too much thyroid hormone. These drugs help to lower the levels of thyroid hormones in the body.

      Antithyroid Drugs are a class of medications used to treat thyroid-related disorders, specifically hyperthyroidism.

      These drugs work by inhibiting the thyroid gland's production of excessive thyroid hormones, helping to restore normal thyroid function.

      They are prescribed to alleviate the symptoms of hyperthyroidism and prepare patients for thyroid surgery or radioactive iodine therapy.

      The common side effects of these drugs are; allergic reactions, decreased WBC, liver problems, and upset stomach.

 

Types: Antithyroid drugs primarily fall into the category of thionamides. Notable representatives include Methimazole and Propylthiouracil (PTU).

• Methimazole (MMI): Methimazole is a thionamide antithyroid drug that effectively inhibits the thyroid gland's production of thyroid hormones.

It is often the preferred choice due to its potency and relatively lower risk of side effects.

It's often the first choice because it works well and usually doesn't cause many problems.

• Propylthiouracil (PTU): This antithyroid drug helps to reduce the thyroid hormone levels by interfering with the synthesis of thyroid hormones, but it's used more in special cases, like during pregnancy when Methimazole might not be the best choice.

 

These medications are used to treat a condition where the thyroid is too active and making too much thyroid hormone. They help to bring things back to normal and reduce the symptoms of having too much thyroid hormone, like a fast heartbeat or feeling jittery.

 

Pharmacological Role:

Antithyroid drugs work by blocking a key process in the thyroid gland. They inhibit an enzyme called thyroperoxidase, which is essential for making thyroid hormones.

By doing this, these drugs slow down the thyroid gland's production of excessive thyroid hormones (T3 and T4).

They act as a control mechanism to bring the thyroid hormone levels back to a healthy, preventing the harmful effects of too much thyroid hormone in the body.Top of Form

 

Clinical Role:

Antithyroid drugs are like "fixers" for thyroid problems.

They're mainly used when your thyroid is overactive and making too much thyroid hormone, causing health issues.

These drugs help bring things back to normal by reducing the excess thyroid hormones.

In some cases, they're used before surgery or special treatments to prepare your thyroid for those procedures.

So, their clinical role is to treat thyroid issues and get your thyroid working right.

 

Side Effects:

Side effects include:- allergic reactions, decreased WBC, liver problems, an upset stomach, or in rare cases joint pain.

 

Define oral hypoglycaemic agents. write its clinical use. describe in simple medical terms.

Definition: HYPO = low, GLYCEMIC = glucose.

Hence medicines that used to decrease the high blood sugar level in body are a

Oral hypoglycemic agents are medications taken by mouth to help lower high blood sugar levels in individuals with diabetes.

They work by various mechanisms to improve the body's utilization of glucose (sugar) and reduce the amount of sugar produced by the liver.

Clinical Use:

Oral hypoglycemic agents are primarily used in the treatment of diabetes mellitus.

These medications are prescribed to:

1. Control Blood Sugar Levels: They help regulate blood glucose levels within a normal range, preventing them from getting too high (hyperglycemia) after eating or too low (hypoglycemia) between meals.
2. Improve Insulin Function: Some of these agents enhance the effectiveness of insulin.
3. Reduce Insulin Resistance: Others work to decrease the body's resistance to insulin, making it easier for cells to respond to insulin's signals.
4. Decrease Sugar Production: Certain oral hypoglycemic agents reduce the liver's production of glucose, helping to prevent excessive sugar release into the bloodstream.
5. Assist in Weight Management: Some medications can help with weight loss, which is often important for individuals with type 2 diabetes.

In Simple Terms:

Oral hypoglycemic agents are pills taken by people with diabetes to help control their blood sugar levels.

They do this by making insulin work better, reducing the body's resistance to insulin, and lowering the amount of sugar the liver produces.

These medications are essential for managing diabetes and keeping blood sugar levels in a healthy range.

 

define histamine. describe its physiological roles. Top of Form

 

    Histamine is a natural chemical substance produced by your body. It plays several roles, related to the immune system and the regulation of various bodily processes.

    histamine is a chemical in your body that has various important functions, including helping with inflammation, allergic reactions, regulating stomach acid, and playing a role in brain function.

    However, an overactive histamine response can lead to problems like allergies and digestive issues.

    Although histamine is small compared to other biological molecules, it plays crucial role in the body.

    It is known to be involved in 23 different philological functions.

    It is columbic {able to carry charge} in nature that allows it to bind more easily.

Its key physiological roles:

1.     Inflammation: Histamine is released when your body detects an injury or infection. It causes blood vessels to expand and become more permeable, allowing immune cells and other substances to reach the affected area quickly. This helps in the healing process but can also lead to symptoms like redness, swelling, and warmth.

 

2.     Allergic Reactions: Histamine is a major player in allergic responses. When you're exposed to an allergen (like pollen or peanuts), your immune system can release histamine, leading to symptoms such as itching, sneezing, runny nose, and hives.

 

3.     Neurotransmission: In the brain, histamine acts as a neurotransmitter, helping to transmit signals between nerve cells. It plays a role in wakefulness, alertness, and regulating sleep cycles.

 

4.     Vasodilation and fall In blood pressure:

 

    It has been known for 100’s of years that an IV injection of histamine leads to vasodilation and decreased blood pressure.

    The underlying mechanism concerts both vasodilation and vascular hyper permeability {causes blood vessels to leak extracellular components and hence dec in blood pressure}.

    Histamine binding to endothelial cells causing them to contract and leads to vascular leak.

    It also stimulates vascular muscle cell relaxants {such as nitric oxide} which causes blood vessel dilation.

    In severe cases, excessive histamine release can result in anaphylactic shock, a life-threatening condition characterized by a rapid drop in blood pressure.

 

Define serotonin and its physiological role.

    Serotonin is a chemical messenger or neurotransmitter in our body that plays several important roles in regulating various bodily functions and emotions.

    serotonin is a natural chemical in your body that affects your mood, sleep, appetite, digestion, and even how your body responds to injuries.

    It plays a crucial role in helping you feel happy and maintaining your body's internal balance.

    Imbalances in serotonin can lead to various health issues, especially in relation to mood and emotions.

Physiological Role of Serotonin:

1.     Mood Regulation:

    Serotonin is often referred to as the "feel-good" neurotransmitter because it helps regulate mood.

    It contributes to feelings of well-being and happiness.

    Imbalances in serotonin levels are associated with conditions like depression and anxiety.

2.     Sleep Regulation:

    Serotonin helps control your sleep-wake cycle.

    It promotes wakefulness during the day and is converted into another neurotransmitter called melatonin at night, which helps regulate sleep.

3.     Appetite and Digestion:

    Serotonin is involved in regulating appetite and digestion.

    It can affect your hunger levels and influence your gut function.

4.     Blood Clotting:

    Serotonin helps regulate blood clotting.

    It can constrict blood vessels and reduce bleeding when you get injured.

5.     Nausea and Vomiting:

    In the gut and brain, serotonin is involved in triggering feelings of nausea and can influence the vomiting reflex.