Pharmacology Chapter 5
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Questions and Answers

Drugs must have the adequate shape so they can bind to their receptors via chemical bonds - the drug shape should be complimentary to that of the ______.

receptor

A drug should be able to reach its site of action after ______.

administration

The drug may be sufficiently soluble and stable to be administered as an ______ drug.

active

A ______ is converted to the active drug inside the body by biological processes.

<p>prodrug</p> Signup and view all the answers

The drug must be ______ at the site of administration - unless the action is local, absorption is usually made into the blood.

<p>absorbed</p> Signup and view all the answers

The drug must be distributed - usually through the blood flow - to its site of ______.

<p>action</p> Signup and view all the answers

The drug may be ______ at any point since absorption.

<p>metabolised</p> Signup and view all the answers

After its effect, the drug should be ______ at a reasonable rate.

<p>eliminated</p> Signup and view all the answers

Isotretinoin causes ______;

<p>cheilitis</p> Signup and view all the answers

Most antifungals inhibit the synthesis of ______ in both yeasts and dermatophytes.

<p>ergosterol</p> Signup and view all the answers

Isotretinoin can lead to ______ due to its drying effects on the skin.

<p>xerosis</p> Signup and view all the answers

One potential side effect of isotretinoin is ______ bleeds.

<p>nose</p> Signup and view all the answers

Imidazoles include drugs like ______ and clotrimazole.

<p>ketoconazole</p> Signup and view all the answers

Lice are treated with rinse-off formulations like creams, foams, and ______.

<p>solutions</p> Signup and view all the answers

Isotretinoin can cause increased serum ______;

<p>lipids</p> Signup and view all the answers

Permethrin is effective against lice at a concentration of ______%.

<p>1</p> Signup and view all the answers

Calcipotriene and calcitriol are ______ analogues applied topically.

<p>vitamin D</p> Signup and view all the answers

Photosensitivity is a side effect of ______.

<p>isotretinoin</p> Signup and view all the answers

Scabies are treated with solutions or lotions that must be applied to the whole body, from the neck ______.

<p>down</p> Signup and view all the answers

Isotretinoin is ______, therefore young females should be given adequate contraception.

<p>teratogenic</p> Signup and view all the answers

Keratolytic agents are applied topically to aid ______ and decrease the symptoms of hyperkeratosis.

<p>desquamation</p> Signup and view all the answers

Temporary worsening of ______ can occur with isotretinoin use.

<p>lesions</p> Signup and view all the answers

Emollients are frequently used in therapy-free periods to minimize skin ______ that can lead to early recurrence.

<p>dryness</p> Signup and view all the answers

Keratolytic agents are often prescription medicines due to their potential as skin ______.

<p>sensitisers</p> Signup and view all the answers

Isotretinoin is commonly prescribed for ______ vulgaris.

<p>acne</p> Signup and view all the answers

Ceramides, cholesterol, and free fatty acids are key components in ______ therapy for barrier restoration.

<p>emollient</p> Signup and view all the answers

Treatment for onychomycosis includes nail ______ containing amorolfine.

<p>lacquer</p> Signup and view all the answers

Soothing agents, such as starch and allantoin, are used to alleviate ______.

<p>itch</p> Signup and view all the answers

To manage retention hyperkeratosis, it is important to prevent the formation of an ______ environment.

<p>anaerobic</p> Signup and view all the answers

Humectants like urea and glycerin are important for maintaining skin ______.

<p>hydration</p> Signup and view all the answers

Topical corticosteroids are used to alleviate most dermatitis-related signs, such as ______ and erythema.

<p>itch</p> Signup and view all the answers

Topical corticosteroids are avoided in seborrhoeic dermatitis due to the influence of ______ spp. yeasts.

<p>Malassezia</p> Signup and view all the answers

Topical treatment is often used for _____ disorders.

<p>skin</p> Signup and view all the answers

The effectiveness of a drug in treating skin disorders can be influenced by _____ variation in drug penetration.

<p>regional</p> Signup and view all the answers

Vehicles and excipients may have _____ effects in the treatment of skin disorders.

<p>therapeutic</p> Signup and view all the answers

_____ agents, emollients, and skin penetration enhancers are used to increase drug permeation.

<p>Occlusive</p> Signup and view all the answers

The type of skin disorder may define the most appropriate _____ for treatment.

<p>vehicle</p> Signup and view all the answers

Topical _____ are used to prevent infections in clean wounds.

<p>antibiotics</p> Signup and view all the answers

In most dermatoses, _____ bacteria are commonly found.

<p>Gram+</p> Signup and view all the answers

Hydrophilic and lipophilic properties are important for _____ formulations.

<p>cream</p> Signup and view all the answers

Drying preparations are often used for inflammatory skin disorders with _____ and crusting.

<p>oozing</p> Signup and view all the answers

The _____ of drug release is an important consideration in drug formulation for skin application.

<p>rate</p> Signup and view all the answers

Bioavailability is defined as the fraction of unchanged drug reaching the ______ circulation.

<p>systemic</p> Signup and view all the answers

In topical administration, bioavailability refers to the fraction of unchanged drug that reaches the site of ______.

<p>action</p> Signup and view all the answers

The area under the concentration curve (AUC, mg.h/L) defines the body’s exposure to the ______.

<p>drug</p> Signup and view all the answers

Half-life (t1/2) is the time required to change the amount of drug in the body by one ______ during elimination.

<p>half</p> Signup and view all the answers

When drug doses are repeated, the drug accumulates in the body until administration ______.

<p>stops</p> Signup and view all the answers

Balancing dose intervals and half-lives is key for effective ______.

<p>treatment</p> Signup and view all the answers

The main factors affecting bioavailability are the extent of absorption, first-pass elimination, and the rate of ______.

<p>absorption</p> Signup and view all the answers

Carrier proteins and endocytosis facilitate the ______ diffusion of drugs across cell membranes.

<p>lipid</p> Signup and view all the answers

Flashcards

Drug Shape

The specific shape of a drug molecule that allows it to bind to a receptor, like a key fitting into a lock.

Pharmacokinetics

The study of how the body affects the drug, including absorption, distribution, metabolism, and excretion.

Pharmacodynamics

The study of how the drug affects the body, including its actions and effects.

Agonist

A drug that binds to a receptor and activates it, initiating a cellular response.

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Antagonist

A drug that binds to a receptor but does not activate it, blocking the action of other agonists.

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Enzymatic Receptors

Receptors that function as enzymes, where a drug can bind and either activate or inhibit the enzyme's activity.

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Prodrug

A drug that is initially inactive but is converted into an active form within the body.

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ADME (Absorption, Distribution, Metabolism, Elimination)

The process of a drug being absorbed into the bloodstream, distributed to its target site, metabolized by the body, and ultimately eliminated.

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Drug Absorption

The process of a drug entering the body and reaching the bloodstream.

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Bioavailability

The fraction of unchanged drug that reaches the systemic circulation.

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Drug Absorption Routes

Pathways by which drugs cross cell membranes during absorption.

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Factors Affecting Bioavailability

Factors influencing the amount of drug that reaches the bloodstream.

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Drug Half-Life (t1/2)

The time it takes for the concentration of a drug in the body to decrease by half.

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Drug Elimination

The process of removing a drug from the body.

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Maintaining Drug Effectiveness

Maintaining effective drug levels in the body by balancing dosing intervals and half-life.

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Area Under the Curve (AUC)

The area under the concentration-time curve (AUC), which reflects the body's exposure to a drug.

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Topical Antifungals

Antifungal medications applied directly to the affected area, often in the form of creams, ointments, solutions, or nail lacquers.

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Onychomycosis

A type of fungal infection that affects the nails, commonly known as nail fungus.

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Skin as a Drug Reservoir

The skin can act as a storage site for certain medications, influencing how the drug is absorbed and eliminated.

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Antifungal Medications

Medications that inhibit the synthesis of ergosterol, a vital component of fungal cell membranes, thereby preventing the growth of fungi.

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Vehicle Effect on Topical Drugs

The way a drug is formulated (ointment, cream, etc.) affects how well it enters the skin and works.

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Fungistatic Agents

Agents that stop or slow the growth of fungi.

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Fungicidal Agents

Agents that kill fungi.

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Regional Variation in Drug Penetration

The amount of drug applied to the skin needs to be adjusted based on the skin area treated.

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Drug Solubility and Vehicle Effects on Release Rate

Factors like the drug's solubility and the vehicle's ability to hydrate the skin impact how quickly the drug releases.

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Dermatophyte infection

A type of fungal infection affecting the skin, hair, and nails.

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Tinea Cruris

A type of fungal infection that affects the skin, commonly found in warm and moist areas like the groin, underarms, and between the toes.

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Concentration Gradient and Drug Penetration

The concentration of the drug in the topical formulation determines how much penetrates the skin.

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Keratolytic agents

Medications applied directly to the skin to remove excess dead skin cells and reduce the buildup of oil in pores, helping to prevent the formation of acne.

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Drying Preparations for Skin Disorders

For skin conditions with inflammation and fluid leakage, drying preparations are often used.

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Lubricating Preparations for Skin Disorders

For skin conditions causing dryness, scaling, and thickness, lubricating preparations are preferred.

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Skin Penetration Enhancers

These are substances that help drugs penetrate the skin more easily.

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Dosage Forms in Dermatology

Ointments, creams, gels, and pastes are common dosage forms used in treating skin disorders.

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Topical Antibiotics for Bacterial Skin Infections

Topical antibiotics are commonly used for treating bacterial infections in the skin.

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Isotretinoin for Acne

A type of acne treatment that involves using a medication like isotretinoin, which is known to be teratogenic (harmful to a developing fetus) and requires careful contraception measures, especially for young women.

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Isotretinoin Side Effects

Isotretinoin, a medication used for severe acne, can cause various side effects, including:

  • Cheilitis (dry, cracked lips)
  • Xerosis (dry skin)
  • Nosebleeds
  • Photosensitivity (increased sensitivity to sunlight)
  • Increased serum lipids (higher cholesterol levels)
  • Temporary worsening of acne lesions
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Isotretinoin and Contraception

Isotretinoin is a medication that can cause severe birth defects, so women of childbearing age must use effective contraception measures, such as hormonal methods or barrier methods, while taking it.

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Inflammatory Dermatoses

A category of skin conditions characterized by inflammation, such as acne, eczema, and psoriasis.

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Vitamin D Analogues in Psoriasis

Vitamin D analogues, like calcipotriene and calcitriol, applied to the skin to slow down the growth of skin cells (keratinocytes) and encourage them to mature properly. They are used in the treatment of psoriasis.

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Emollients in Skincare

Moisturizing agents used to help protect the skin and prevent dryness, which can worsen skin conditions like eczema. They act by restoring and maintaining the skin's natural barrier.

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Humectants

A type of emollient that helps maintain skin moisture by attracting and holding water within the skin. Examples include urea and glycerin.

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Occlusives

Emollients that create a barrier on the skin to prevent water loss. They help seal in moisture and protect the skin from environmental irritants.

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Soothing Agents

Agents that reduce itch or irritation. Examples include starch, allantoin, and ectoin, which are often used in eczema treatment.

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Dermatitis

A type of skin condition that causes inflammation, redness, and itching. It is often characterized by scaly patches and can occur in different forms.

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Topical Corticosteroids in Dermatitis

Corticosteroids are potent anti-inflammatory drugs used topically to reduce inflammation, redness, and itch in many types of dermatitis. They are, however, generally not recommended for seborrheic dermatitis, due to the role of Malassezia yeasts in this condition.

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Study Notes

Advanced Cosmetic Science - Introduction to Pharmacology, Dermopharmacy and Cosmetics

  • Pharmacology: The study of substances interacting with living systems via chemical processes, by activating or inhibiting normal bodily processes.

  • Drug: Any substance used for diagnosis, disease prevention, or therapeutic purposes. It modifies physiological or pathological states for the recipient's benefit.

  • Chemical Actions: Drugs work through chemical actions.

  • Drug Receptors: Specific molecules facilitating drug action.

  • Drug Size: Drug molecule sizes vary widely, from tiny to very large (proteins). Most drugs have molecular weights (Mw) between 100 and 1000. A molecule's unique shape and charge are vital for binding to a specific receptor, preventing binding to other receptors. Sufficient size is needed for uniqueness. Drugs need to move within the body; large molecules don't diffuse easily between body compartments.

  • Drug Shape: Drug shape must be complementary to the receptor shape for effective binding via chemical bonds.

  • Pharmacokinetics: The process describing how drugs are absorbed, distributed, metabolized, and eliminated (ADME) in the body. A drug must reach its site of action after administration.

  • Absorption: The drug must be absorbed into the bloodstream (except in local applications).

  • Distribution: Drugs are distributed by blood flow to the target area, passing through barriers separating body compartments.

  • Metabolism: Drug metabolism happens at any point after absorption.

  • Elimination: The drug must be eliminated at a reasonable rate after the action is complete.

  • Bioavailability: The fraction of unchanged drug reaching the systemic circulation.

  • Half-life (t1/2) : The time it takes for the amount of drug in the body to reduce by half during elimination. Dose intervals and half-lives are key to effective treatment. Repeated drug doses lead to accumulation until dosing stops.

  • Drug Size: Factors impacting bioavailability are the extent of absorption, first-pass elimination, and the rate of absorption. The area under the concentration curve (AUC) measures the total exposure of the body to a drug.

  • Drug Shape: Different drug administration routes (e.g., intravenous, intramuscular, subcutaneous, oral, rectal, inhalation, transdermal) have different bioavailability percentages.

  • Pharmacodynamics: The study of how drugs interact with their targets (e.g., receptors and enzymes) to produce their effects. Agents can be agonists (producing the same effect as the natural chemical messenger) or antagonists (blocking the natural chemical messenger's effects). Enzymes can be blocked, inhibiting the normal function.

  • Drug-Receptor Interactions: Drugs bring about changes in biological functions through their chemical actions. Receptors are specific molecules in the target biological system that play regulatory roles. Examples include lidocaine blocking pain signals through Na+ channels.

  • Enzymatic Receptors: Drugs can also affect enzymatic activities. For example, a drug might block an enzyme’s active site, thus inhibiting its activity.

  • Drugs/Receptors: Drugs can interact with receptors. For instance, lidocaine blocks sodium channels to stop pain signals.

  • A Prodrug: An inactive precursor enabling easier absorption and distribution.

  • Pharmacokinetic Principles: Drug stability and solubility are critical for effective administration.

  • Treatment of Skin Disorders: Skin disorders are treated systemically or topically. Variables influencing response include regional variation in penetration, dosing schedule, vehicle used (and whether it causes occlusion), and drug concentration gradients. Skin can act as a reservoir for some drugs. Vehicles and excipients contribute to drug effects.

  • Treatment of Infectious Dermatoses: Topical antibiotics, antibiotic selection depending on bacteria type, early treatment, and considerations on clean wounds, are important components of topical antibiotic treatment. Typical examples include bacitracin (Gram+), clindamycin (gram-positive and negative), metronidazole (acne and rosacea), and tetracyclines (severe acne).

  • Treatment of Viral Dermatoses: Many viral warts resolve, though antiviral treatment can accelerate healing for herpes simplex or zoster. Cryotherapy, salicylic acid, and surgical removal methods for removal of warts.

  • Treatment of Fungal Dermatoses: Antifungals (imidazoles, nystatin) inhibit ergosterol synthesis.

  • Treatment of Parasitic Dermatoses: Lice are treated with rinse-off formulations containing agents like permethrin. Scabies requires body-wide treatment with lotions/solutions, and follow-up washing.

  • Treatment of Inflammatory Dermatoses: Acne is frequently associated with issues such as retention hyperkeratosis, excessive sebum, and comedogenic materials. Methods to treat inflammatory dermatoses include keratolytic agents, to manage sebum, and to target comedones.

  • Treatment of Dermatitis: Topical corticosteroids are useful anti-inflammatory agents for eczema, acne, and psoriasis.

  • Treatment of Dyschromias: Hypermelanosis and hypomelanosis treatments include skin lightening agents, UV protection, tyrosinase inhibitors, and topical corticosteroid use (with possible side effects).

Subheadings

  • Note that subheadings in the provided document are not always present or properly used - I've attempted to organize the information in a coherent manner.

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Test your knowledge on the key concepts of pharmacology, especially regarding drug action, absorption, and effects. This quiz covers essential topics such as drug shape, administration, and side effects. Get ready to explore the fascinating world of how drugs interact within the body!

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