Podcast
Questions and Answers
A topical drug's ability to penetrate the skin and enter systemic circulation is LEAST affected by which factor?
A topical drug's ability to penetrate the skin and enter systemic circulation is LEAST affected by which factor?
- Molecular size facilitating penetration for smaller molecules.
- Presence of a compromised skin barrier, such as inflamed skin.
- The drug's color influencing absorption rates. (correct)
- High lipophilicity promoting easier penetration.
A drug with a higher pKa value is more likely to:
A drug with a higher pKa value is more likely to:
- Exist in an ionized state and penetrate the skin easily.
- Be hydrophilic and enter systemic circulation slowly.
- Be structurally complex and penetrate the skin rapidly.
- Exist in a non-ionized state and penetrate the skin easily. (correct)
Why are topical steroids more likely to enter the systemic circulation when applied to inflamed skin?
Why are topical steroids more likely to enter the systemic circulation when applied to inflamed skin?
- Inflammation enhances the drug's lipophilic properties.
- Inflammation increases the drug's ionization, promoting absorption.
- Inflammation compromises the skin barrier, increasing penetrability. (correct)
- Inflammation decreases local blood flow, concentrating the drug.
What is the MOST critical factor determining the systemic absorption of a topically applied drug?
What is the MOST critical factor determining the systemic absorption of a topically applied drug?
How do delivery methods influence the pharmacokinetics of topical drugs?
How do delivery methods influence the pharmacokinetics of topical drugs?
A patient presents with skin necrosis induced by warfarin. What is the MOST likely mechanism by which warfarin leads to this adverse effect?
A patient presents with skin necrosis induced by warfarin. What is the MOST likely mechanism by which warfarin leads to this adverse effect?
What strategies can be used in the management of acne vulgaris?
What strategies can be used in the management of acne vulgaris?
How does benzoyl peroxide reduce acne?
How does benzoyl peroxide reduce acne?
A patient with moderate acne vulgaris has been using topical tretinoin for several weeks with limited improvement. The physician is considering adding another retinoid. Which of the following retinoids would be MOST appropriate, considering its side effect profile and potency?
A patient with moderate acne vulgaris has been using topical tretinoin for several weeks with limited improvement. The physician is considering adding another retinoid. Which of the following retinoids would be MOST appropriate, considering its side effect profile and potency?
How do retinoid-based drugs such as tretinoin and isotretinoin function at the cellular level to treat acne?
How do retinoid-based drugs such as tretinoin and isotretinoin function at the cellular level to treat acne?
Tretinoin is used to manage acute promyelocytic leukemia (APL) because it:
Tretinoin is used to manage acute promyelocytic leukemia (APL) because it:
Which of the following is the MOST accurate statement regarding adapalene when compared to other retinoids?
Which of the following is the MOST accurate statement regarding adapalene when compared to other retinoids?
For which patient population is isotretinoin strictly contraindicated?
For which patient population is isotretinoin strictly contraindicated?
A patient is prescribed isotretinoin for severe acne. Regular monitoring of which lab values is MOST critical to ensure patient safety?
A patient is prescribed isotretinoin for severe acne. Regular monitoring of which lab values is MOST critical to ensure patient safety?
What is a potential consequence of using retinoid-based drugs during pregnancy?
What is a potential consequence of using retinoid-based drugs during pregnancy?
What is the primary mechanism by which azelaic acid manages acne?
What is the primary mechanism by which azelaic acid manages acne?
Why is azelaic acid's metabolism unique compared to many other drugs?
Why is azelaic acid's metabolism unique compared to many other drugs?
Which of the following is a reason why finasteride is considered an 'OFF-LABEL' treatment for acne vulgaris in women?
Which of the following is a reason why finasteride is considered an 'OFF-LABEL' treatment for acne vulgaris in women?
What is a potential adverse effect of finasteride use in males?
What is a potential adverse effect of finasteride use in males?
Why is spironolactone sometimes used off-label to treat acne in women?
Why is spironolactone sometimes used off-label to treat acne in women?
Which cells and cytokines are MOST directly involved in the formation of atopic dermatitis (eczema)?
Which cells and cytokines are MOST directly involved in the formation of atopic dermatitis (eczema)?
Which of the following represents the correct order of increasing potency for topical corticosteroids?
Which of the following represents the correct order of increasing potency for topical corticosteroids?
How does topical tacrolimus alleviate atopic dermatitis symptoms?
How does topical tacrolimus alleviate atopic dermatitis symptoms?
What is the primary mechanism by which dupilumab acts in the management of atopic dermatitis?
What is the primary mechanism by which dupilumab acts in the management of atopic dermatitis?
Systemic corticosteroids are reserved for treating atopic dermatitis only when:
Systemic corticosteroids are reserved for treating atopic dermatitis only when:
A patient presents with a bluish discoloration secondary to amiodarone use. Which mechanism BEST explains this discoloration?
A patient presents with a bluish discoloration secondary to amiodarone use. Which mechanism BEST explains this discoloration?
A patient develops drug-induced lupus secondary to hydralazine. What is the MOST likely underlying mechanism for this adverse reaction?
A patient develops drug-induced lupus secondary to hydralazine. What is the MOST likely underlying mechanism for this adverse reaction?
A patient taking doxycycline develops photodermatosis. Which of the following strategies would be LEAST effective in managing this condition?
A patient taking doxycycline develops photodermatosis. Which of the following strategies would be LEAST effective in managing this condition?
A patient who is on long-term warfarin therapy develops skin necrosis. What underlying process involving coagulation factors is MOST likely contributing to this condition?
A patient who is on long-term warfarin therapy develops skin necrosis. What underlying process involving coagulation factors is MOST likely contributing to this condition?
A patient with acne vulgaris is prescribed benzoyl peroxide. What is the MOST relevant mechanism by which benzoyl peroxide achieves its therapeutic effect?
A patient with acne vulgaris is prescribed benzoyl peroxide. What is the MOST relevant mechanism by which benzoyl peroxide achieves its therapeutic effect?
A patient with severe acne is prescribed isotretinoin. What is the MOST important reason to monitor hepatic labs regularly during isotretinoin therapy?
A patient with severe acne is prescribed isotretinoin. What is the MOST important reason to monitor hepatic labs regularly during isotretinoin therapy?
A female patient is considering finasteride as an off-label treatment for acne vulgaris. What is the MOST critical consideration regarding the use of finasteride in women?
A female patient is considering finasteride as an off-label treatment for acne vulgaris. What is the MOST critical consideration regarding the use of finasteride in women?
For what specific type of patient is spironolactone mostly used off-label?
For what specific type of patient is spironolactone mostly used off-label?
Aside from genetics, what of the following will MOST affect a person's likelihood of skin penetration?
Aside from genetics, what of the following will MOST affect a person's likelihood of skin penetration?
Of the following options, which BEST describes how delivery method affect topical drugs?
Of the following options, which BEST describes how delivery method affect topical drugs?
How do retinoid-based drugs treat acne?
How do retinoid-based drugs treat acne?
Which class of drugs is NOT able to be used during pregnancy?
Which class of drugs is NOT able to be used during pregnancy?
A novel topical medication is developed with a molecular weight of 600 Daltons and a logP value of 4.5. Considering these characteristics, which of the following strategies would MOST effectively enhance its penetration through the stratum corneum?
A novel topical medication is developed with a molecular weight of 600 Daltons and a logP value of 4.5. Considering these characteristics, which of the following strategies would MOST effectively enhance its penetration through the stratum corneum?
A researcher is comparing the efficacy of different topical corticosteroids in treating eczema. Drug X has a fluorinated structure, while Drug Y is non-fluorinated. Assuming both are applied in equivalent concentrations and formulations, which statement BEST predicts their relative potencies and systemic absorption?
A researcher is comparing the efficacy of different topical corticosteroids in treating eczema. Drug X has a fluorinated structure, while Drug Y is non-fluorinated. Assuming both are applied in equivalent concentrations and formulations, which statement BEST predicts their relative potencies and systemic absorption?
A female patient with moderate acne vulgaris who has not responded to topical retinoids and benzoyl peroxide is considering off-label use of finasteride. Which of the following hormonal profiles would be MOST indicative of potential benefit and reduced risk from finasteride therapy?
A female patient with moderate acne vulgaris who has not responded to topical retinoids and benzoyl peroxide is considering off-label use of finasteride. Which of the following hormonal profiles would be MOST indicative of potential benefit and reduced risk from finasteride therapy?
A patient with severe atopic dermatitis is being treated with dupilumab. After several months, the patient reports significant improvement in skin lesions but develops new-onset conjunctivitis and complains of persistent itching. Which of the following BEST explains these findings?
A patient with severe atopic dermatitis is being treated with dupilumab. After several months, the patient reports significant improvement in skin lesions but develops new-onset conjunctivitis and complains of persistent itching. Which of the following BEST explains these findings?
A patient presents with skin necrosis after starting warfarin therapy. Further investigation reveals a deficiency in protein C. Which of the following BEST describes the mechanism by which warfarin contributes to skin necrosis in this patient?
A patient presents with skin necrosis after starting warfarin therapy. Further investigation reveals a deficiency in protein C. Which of the following BEST describes the mechanism by which warfarin contributes to skin necrosis in this patient?
Flashcards
Lipophilic Drugs
Lipophilic Drugs
Drugs that are highly lipophilic enter the systemic circulation more easily.
Molecular Size and Penetration
Molecular Size and Penetration
Smaller molecules penetrate the skin more easily than larger, complex molecules.
Ionization of Drugs
Ionization of Drugs
Non-ionized drugs are more lipophilic and penetrate the skin more easily. Drugs with higher pKa values are more likely to be in a non-ionized state.
Inflamed Skin and Absorption
Inflamed Skin and Absorption
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Delivery Methods
Delivery Methods
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Acne Vulgaris Management
Acne Vulgaris Management
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First-Line Acne Drugs
First-Line Acne Drugs
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Benzoyl Peroxide Mechanism
Benzoyl Peroxide Mechanism
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Retinoid-Based Drugs
Retinoid-Based Drugs
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Retinoid Mechanism
Retinoid Mechanism
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Results of Retinoid Action
Results of Retinoid Action
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Tretinoin's Unique Use
Tretinoin's Unique Use
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Adapalene
Adapalene
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Isotretinoin facts
Isotretinoin facts
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Azelaic Acid
Azelaic Acid
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Azelaic acid chemical structure
Azelaic acid chemical structure
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Finasteride
Finasteride
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Finasteride in males
Finasteride in males
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Aldosterone
Aldosterone
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formation of atopic dermatitis
formation of atopic dermatitis
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increasing potency
increasing potency
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Tacrolimus
Tacrolimus
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Dupilumab
Dupilumab
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Prednisone
Prednisone
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Study Notes
Pharmacologic Factors of Topical Agents
- Highly lipophilic drugs enter systemic circulation easier than polar/hydrophilic drugs, like topical steroids
- Smaller drug molecules penetrate easier than larger, complex molecules
- Drugs with higher pKa values tend to be non-ionized
- Non-ionized drugs are lipophilic and easily penetrate the skin to enter systemic circulation, e.g., topical salicylic acid
- Inflamed skin has a compromised barrier function and is more penetrable
- Drugs, like topical steroids, are more likely to enter systemic circulation in inflamed skin
- Delivery methods/vehicles like creams, ointments, gels, and patches increase drug penetration and control delivery rates
Acne Vulgaris Management Strategies
- Reduce sebum release from sebaceous glands
- Decrease androgen release from the adrenal cortex (zona reticularis)
- Reduce testosterone to DHT conversion via 5-alpha reductase inhibition
First-Line Acne Vulgaris Drugs
- Benzoyl Peroxide
- Retinoid-Based Drugs
Benzoyl Peroxide Mechanism
- Releases free-radical oxygen to oxidize bacterial proteins in sebaceous follicles, reducing anaerobic bacteria like propionibacterium acnes, and irritating free fatty acids
- It converts to benzoic acid in the skin, then is renally eliminated
Important Retinoid-Based Drugs
- Tretinoin
- Isotretinoin
- Adapalene
Retinoid-Based Drugs Action
- They are Vitamin A derivatives
- They enter keratinocytes and bind to RARs (retinoic acid receptors) which are nuclear transcription factors, inducing changes in gene expression, leading to increased terminal differentiation and inhibited proliferation
- Results in decreased pore clogging by removing keratinocytes, reduced sebum production, and decreased comedone formation
Pharmacologic Considerations: Tretinoin
- Can manage Acute Promyelocytic Leukemia
- It involves a unique mutation with a hyper-proliferative oncogene with the retinoic acid receptor
- By blocking the RAR activity, proliferation of cancerous myeloid cells is reduced
Pharmacologic Considerations: Adapalene
- Has a more favorable side effect profile than other retinoids
- Less potent than tretinoin/isotretinoin
Pharmacologic Considerations: Isotretinoin
- Is extremely potent, but carries a large adverse effect profile
- It requires serial monitoring of hepatic labs (serum transaminases, cholesterol, lipids) because of hepatotoxicity risk
- Contraindicated in cirrhosis/liver failure patients
- Active metabolite: 4-oxo-isotretinoin
Retinoid-Based Drugs in Pregnancy
- They are contraindicated
Azelaic Acid Acne Management
- Exhibits three primary mechanisms
- It is a bacteriostatic agent, it stops Propionibacterium proliferation by interfering with RNA and DNA polymerase
- Acts as an anti-inflammatory by destroying free radicals/reactive oxygen species and decreasing pro-inflammatory cytokines, reducing comedone formation and skin inflammation
- Prevents comedone formation by promoting terminal differentiation in hair follicles and clearing follicles to reduce comedones
Azelaic Acid Properties
- Azelaic acid is dicarboxylic
- It metabolizes via beta-oxidation and is broken down into smaller carboxylic acid units, eliminated renally
Off-Label Acne Interventions: Finasteride (Females only)
- Finasteride is a 5-alpha reductase inhibitor that reduces DHT, a trigger for sebum production
- Anti-androgenic effects make it a useful off-label acne treatment for women
- Can lead to gynecomastia, testicular atrophy, decreased penile length, decreased libido in males
Off-Label Acne Interventions: Aldosterone (Females only)
- Aldosterone is an aldosterone receptor antagonist
- It demonstrates anti-androgenic effects by suppressing 5-alpha reductase, reducing DHT, and suppressing androgen production in ovaries/adrenal glands
- Can lead to gynecomastia, testicular atrophy, decreased penile length, decreased libido in males
- Spironolactone has electrolyte-based adverse effects
Atopic Dermatitis Immunologic Players
- Th2 CD4 T cells
- B lymphocytes producing IgE
- Basophils, mast cells, eosinophils
- Pro-inflammatory cytokines like IL-4 that promotes IgE production and IL-13 that promotes fibrosis, itching associates with atopic dermatitis
Atopic Dermatitis Pharmacologic Management
- First line treatment is topical corticosteroids: hydrocortisone, triamcinolone, betamethasone
- Increasing potency: hydrocortisone, triamcinolone, betamethasone
- Tacrolimus targets calcineurin
- Calcineurin inhibition, inhibits a kinase that activates T lymphocytes, which then decreases Th2 CD4 T cell activation
- This results in less IgE production and reduced eosinophil, basophil, and mast cell recruitment, which mitigates atopic dermatitis
- Dupilumab
- IL-4 receptor blockade decreases Th2 CD4 T cell upregulation, reducing IgE production and eosinophil, basophil, and mast cell recruitment
- IL-13 receptor blockade decreases cytokine expresssion, thus reducing itch and skin inflammation, patients MUST be monitored for parasitic infections
- Prednisone and Prednisolone only for systemic involvement
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