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Year 2 Medicine > Hormonal Drug Delivery > Flashcards

Hormonal Drug Delivery Flashcards

1
Q

… forms are essentially pharmaceutical products in the form in which they are marketed for …

A

Dosage forms are essentially pharmaceutical products in the form in which they are marketed for use

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2
Q

Pharmaceutics is the science of turning a … into a … form

A

Pharmaceutics is the science of turning a drug into a dosage form

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3
Q

Examples of dosage forms

A
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4
Q

Why do we have dosage forms?

  • Drug often comes in … form
  • … doses of drug
    • e.g. mg or μg quantities
  • Bulk up with …
    • such as w.., l.. etc..
A
  • Drug often comes in powder form
  • Tiny doses of drug
    • mg or μg quantities
  • Bulk up with excipients
    • such as water, lactose etc..
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5
Q

Why do we have different dosage forms?

    1. Different … conditions
    1. Different … of …
    1. Different … of …
    1. Different … properties of drug
A
    1. Different clinical conditions
    1. Different types of patient
    1. Different routes of administration
    1. Different physicochemical properties of drug
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6
Q

Why do we have different dosage forms? - 1) Different Clinical Conditions

  • e.g. a rash can be treated by a … but an emergency or a seizure needs a dosage form that works … such as an … or a s… (if cannot swallow).
A
  • e.g. a rash can be treated by a cream but an emergency or a seizure needs a dosage form that works rapidly such as an injection or a suppository (if cannot swallow).​
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7
Q

Why do we have different dosage forms? - 2) Different Types of Patient

A
  • Elderly vs Child
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8
Q

Why do we have different dosage forms? - 3) Different Routes of …

A
  • administration
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9
Q

Why do we have different dosage forms? - 4) Different Physiocochemical Properties

  • e.g. if a drug is not active … because it cannot pass through … … it needs to be formulated as an … e.g. insulin (which is also broken down by stomach enzymes)
A
  • e.g. if a drug is not active orally because it cannot pass through cell membranes it needs to be formulated as an injection e.g. insulin (which is also broken down by stomach enzymes)
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10
Q

Factors to Consider when Designing Dosage Forms

    1. … factors
      * Solubility, partition coefficient, pKa, stability, molecular weight
    1. … factors
      * Absorption, bioavailability, route of administration
    1. … factors
      * Disease, patient, route, local vs. systemic delivery
A
    1. Drug factors
      * Solubility, partition coefficient, pKa, stability, molecular weight
    1. Biopharmaceutical factors
      * Absorption, bioavailability, route of administration
    1. Therapeutic factors
      * Disease, patient, route, local vs. systemic delivery
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11
Q

What 3 Factors do we need to consider when designing Dosage Forms?

A
    1. Drug factors
      * Solubility, partition coefficient, pKa, stability, molecular weight
    1. Biopharmaceutical factors
      * Absorption, bioavailability, route of administration
    1. Therapeutic factors
      * Disease, patient, route, local vs. systemic delivery
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12
Q

Main routes of administration

A
  1. Oral or Peroral (swallowed by mouth)
  2. Oral cavity (absorbed from mouth, but not swallowed)
    • Oral mucosa
    • Buccal (between gum and cheek)
    • Sublingual (from under the tongue)
  3. Rectal
  4. Parenteral (injected)
  5. Epicutaneous (skin) – including topical or transdermal
  6. Ocular (eye), aural (ear), nasal (nose)
  7. Pulmonary (lungs)
  8. Vaginal
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13
Q

Main route of administration is …

A

oral or peroral (Swallowed by mouth)

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14
Q

Oral cavity administration includes: (3)

A
  • oral mucosa
  • buccal (between gum and cheek)
  • sublingual (from under the tongue)
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15
Q

Parenteral route of administration means…

A

injected

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16
Q

Epicutaneous route of administration means …

A

skin - including topical or transdermal

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17
Q

ocular administration …

A

eye

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18
Q

aural administration …

A

ear

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19
Q

nasal administration …

A

nose

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20
Q

pulmonary administration …

A

lungs

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21
Q

Local Delivery

  • Site of administration = site of …
  • … onset of action
  • … drug required
  • Absorption into the … … is not required (but some absorption could occur)
    • Absorption into the … … can lead to … … …
A
  • Site of administration = site of action
  • Rapid onset of action
  • Less drug required
  • Absorption into the blood stream is not required (but some absorption could occur)
    • Absorption into the blood stream can lead to unwanted side effects
22
Q

Systemic delivery

  • Effect results from entry of drug into … system
  • Drug transported to site of action in the …
  • Drug can be placed … in …
    • E.g. by … injection
  • Or … into bloodstream
    • Following … or other route of administration
A
  • Effect results from entry of drug into circulatory system
  • Drug transported to site of action in the blood
  • Drug can be placed directly in bloodstream
    • E.g. by intravenous injection
  • Or absorbed into bloodstream
    • Following oral or other route of administration
23
Q

Systemic delivery: bioavailability

  • Bioavailability relates to the … and … of drug absorption into the blood.
A
  • Bioavailability relates to the RATE and EXTENT of drug absorption into the blood.
24
Q

Consider the duration of action

  • E.g. painkiller for headache - dose, increase in drug concentration and decrease again
  • To give drug all the time - … oral … regimen - give second dose before concentration has decreased again to maintain drug in … window
A
  • E.g. painkiller for headache - dose, increase in drug concentration and decrease again
  • To give drug all the time - multiple oral dosing regimen - give second dose before concentration has decreased again to maintain drug in therapeutic window
25
Q

Types of hormones

  • Modified amino acid derivatives (derived from tyrosine or tryptophan) e.g. d.., t…
  • Peptide and proteins (derived from amino acids) e.g. neuropeptides (v..), pituitary hormones (g…), GI hormones (insulin)
  • Steroids (derived from c…) e.g. sex hormones (t…), corticosteroids (hydro…)
  • Eicosanoids (derived from l…) e.g. prostaglandins, leukotrienes
A
  • Modified amino acid derivatives (derived from tyrosine or tryptophan) e.g. dopamine, thyroxine
  • Peptide and proteins (derived from amino acids) e.g. neuropeptides (vasopressin), pituitary hormones (gonadotropins), GI hormones (insulin)
  • Steroids (derived from cholesterol) e.g. sex hormones (testosterone), corticosteroids (hydrocortisone)
  • Eicosanoids (derived from lipids) e.g. prostaglandins, leukotrienes
26
Q

Modified amino acid derivatives e.g. thyroxine and corticosteroids e.g. hydrocortisone

  • Drug factors
    • … dose required
  • Biopharmaceutical factors – which route?
    • … bioavailable
  • Therapeutic factors
    • … vs. … delivery
A
  • Drug factors
    • Low dose required
  • Biopharmaceutical factors – which route?
    • Orally bioavailable
  • Therapeutic factors
    • Local vs. systemic delivery
27
Q

Dose of drug - small e.g. 25microgram thyroxine

  • E… such as:
    • Diluents/fillers e.g. lactose, water
    • Lubricants e.g. Mg stearate
    • Disintegrants e.g. starch
    • Surfactants e.g. polysorbates
    • Viscosity enhancing agents e.g. cellulose derivatives
    • Flavours, colours, perfumes
    • Sweetening agents
    • Preservatives
A
  • Excipients such as:
    • Diluents/fillers e.g. lactose, water
    • Lubricants e.g. Mg stearate
    • Disintegrants e.g. starch
    • Surfactants e.g. polysorbates
    • Viscosity enhancing agents e.g. cellulose derivatives
    • Flavours, colours, perfumes
    • Sweetening agents
    • Preservatives
28
Q

Local Delivery of Corticosteroids

  • To avoid … side effects need many different dosage forms:
    • Intra-… injections – tennis elbow
    • C.. and O… - eczema
    • I… - asthma
    • … drops - inflammation
    • S… - haemorrhoids
A
  • To avoid systemic side effects need many different dosage forms:
    • Intra-articular injections – tennis elbow
    • Creams and ointments - eczema
    • Inhalers - asthma
    • Eye drops - inflammation
    • Suppositories - haemorrhoids
29
Q

Peptide hormone e.g. Insulin

    1. Drug factors
      * Peptide hormone, … molecule MW ~5800 Da
    1. Biopharmaceutical factors
      * Not … after … administration
    1. Therapeutic factors
      * Need … action
      * Aim to mimic insulin secretion by normal pancreas
      • b.. and b..
A
    1. Drug factors
      * Peptide hormone, large molecule MW ~5800 Da
    1. Biopharmaceutical factors
      * Not absorbed after oral administration
    1. Therapeutic factors
      * Need systemic action
      * Aim to mimic insulin secretion by normal pancreas
      • basal and bolus
30
Q

Insulin Administration

  • Insulin is injected …
A
  • Insulin is injected subcutaneously
31
Q

Insulins characterised by differences in:

  • O…
    • How … they act
  • Peak
    • How quickly they achieve … …
  • D..
    • How long they …
  • Route of delivery
    • s…, i..
A
  • Onset
    • How quickly they act
  • Peak
    • How quickly they achieve maximum impact
  • Duration
    • How long they last
  • Route of delivery
    • Subcutaneous, inhaled
32
Q

Long acting insulin:

  • Provides … insulin
  • Insulin detemir (Levemir®) or insulin glargine (Lantus®)
  • Injected … or … daily
  • Formulated so that the insulin is … water soluble, making it self … and precipitate into microcrystals which act as a depot releasing the insulin … over time.
A
  • Provides baseline insulin
  • Insulin detemir (Levemir®) or insulin glargine (Lantus®)
  • Injected once or twice daily
  • Formulated so that the insulin is less water soluble, making it self aggregate and precipitate into microcrystals which act as a depot releasing the insulin slowly over time.
33
Q

What is Continuous subcutaneous insulin infusion (CSII) of rapid analog?

A
34
Q

Pulmonary Route: Mainly for local delivery but…

  • Can also be used for … delivery
  • … surface area (80 – 140 m2)
  • … epithelial barrier (0.1 – 0.2 μm)
  • Good … supply (100% … output)
  • Avoids harsh environment of … …
  • Avoids …-… hepatic metabolism
    *
A
  • Can also be used for systemic delivery
  • Large surface area (80 – 140 m2)
  • Thin epithelial barrier (0.1 – 0.2 μm)
  • Good blood supply (100% cardiac output)
  • Avoids harsh environment of GI tract
  • Avoids first-pass hepatic metabolism
35
Q

Inhaled Insulin - Afrezza (June 2014 FDA)

  • …-acting inhaled insulin
  • Taken at the beginning of each …
  • Used in combination with a …-acting … insulin
A
  • Rapid-acting inhaled insulin
  • Taken at the beginning of each meal
  • Used in combination with a long-acting injected insulin
36
Q

Sex Hormones

    1. Drug factors
      * S.., Lipo…, MW ~270 Da
    1. Biopharmaceutical factors
      * … absorption after oral administration
      * Extensive first pass … metabolism, … half life.
    1. Therapeutic factors
      * … delivery required but oral route not always ideal
      * Either cyclical or continuous administration required
A
    1. Drug factors
      * Steroid, lipophilic, MW ~270 Da
    1. Biopharmaceutical factors
      * Variable absorption after oral administration
      * Extensive first pass hepatic metabolism, short half life.
    1. Therapeutic factors
      * Systemic delivery required but oral route not always ideal
      * Either cyclical or continuous administration required
37
Q

Need alternatives to oral route

  • To increase … and to offer … release need alternatives to oral route.
  • Systemic delivery
    • … route – intramuscular (IM) injection, implants • Transdermal route - patch or gel
    • … route - spray
    • … route – mucoadhesive system
    • … – gel
A
  • To increase bioavailability and to offer sustained release need alternatives to oral route.
  • Systemic delivery
    • Parenteral route – intramuscular (IM) injection, implants • Transdermal route - patch or gel
    • Intranasal route - spray
    • Buccal route – mucoadhesive system
    • Vaginal – gel
38
Q

IM injections of testosterone/progesterone

    • Testosterone - use … injections – sustained release
      * Testosterone enanthate (in … …)
      * Testosterone decanoate, isocaproate, phenylproprionate, propionate and undecanoate
      • Progesterone - use … – sustained release
        • Nexplanon (progestogen- only …)
A
  • Testosterone - use Oily injections – sustained release
    • Testosterone enanthate (in caster oil)
    • Testosterone decanoate, isocaproate, phenylproprionate, propionate and undecanoate
  • Progesterone - use Implants – sustained release
    • Nexplanon (progestogen- only contraception)
39
Q

Sustanon 250 is used in adult men for … replacement to treat various health problems caused by a lack of … (male …)

A

Sustanon 250 is used in adult men for testosterone replacement to treat various health problems caused by a lack of testosterone (male hypogonadism).

40
Q

Testosterone Esters (Sustanon 250)

  • Esters have … water solubility/… oil solubility
  • But the ester deactivates molecule (can’t … to androgen receptor)
  • Ester is C…/ H… in blood – this restores the OH group, restoring activity.
A
  • Esters have lower water solubility/higher oil solubility
  • But the ester deactivates molecule (can’t bind to androgen receptor)
  • Ester is cleaved/ hydrolysed in blood – this restores the OH group, restoring activity.
41
Q

Release of steroid molecule from oily depots of long chain esters in muscle tissue

  • Sustained action due to lower partition from … phase to … environment of tissue
  • Testosterone ester is hydrolysed at the surface of the droplet, slowly releasing active testosterone.
  • Released over …-… weeks
A
  • Sustained action due to lower partition from oily phase to aqueous environment of tissue
  • Testosterone ester is hydrolysed at the surface of the droplet, slowly releasing active testosterone.
  • Released over 2-3 weeks
42
Q

Subdermal Implant of Etonorgestrel (Nexplanon)

  • … contraceptive – effective for up to … years!
  • Delivered by sub-dermal implantation
A
  • Progesterone only contraceptive – effective for up to 3 years!
  • Delivered by sub-dermal implantation
43
Q

Transdermal Delivery of Estradiol - Systemic Delivery

A
44
Q

Intranasal Administration - Systemic Delivery

  • Advantages
    • … surface area (~180 cm2)
    • Highly …
    • Avoids … … … metabolism
    • Good … for low MW compounds
  • Disadvantages
    • M… clearance
    • M… activity
    • Poor … for high MW compounds
    • Product on the market: Desmopressin
A
  • Advantages
    • Large surface area (~180 cm2)
    • Highly vascularized
    • Avoids first pass hepatic metabolism
    • Good bioavailability for low MW compounds
  • Disadvantages
    • Mucociliary clearance
    • Metabolic activity
    • Poor bioavailability for high MW compounds
    • Product on the market: Desmopressin
45
Q

Buccal Administration - Systemic Delivery

  • Mucoadhesive t… buccal delivery system
  • Applied … daily
  • Adheres to … or inner …
  • … release of … through buccal mucosa
A
  • Mucoadhesive testosterone buccal delivery system
  • Applied twice daily
  • Adheres to gum or inner cheek
  • Sustained release of testosterone through buccal mucosa
46
Q

Vaginal Administration - Systemic Delivery

  • …-insertion and removal
  • … release
  • … patient compliance
  • Used to assist …
  • B… vaginal gel (Crinone)
  • Progesterone released over ..-..h
A
  • Self-insertion and removal
  • Continuous release
  • Good patient compliance
  • Used to assist reproduction
  • Bioadhesive vaginal gel (Crinone)
  • Progesterone released over 25-50h
47
Q

Vaginal Administration (device) - Local Delivery

  • Vaginal … (Estring)
  • Estradiol released over … days
  • Used in … atrophy of the vagina
A
  • Vaginal ring (Estring)
  • Estradiol released over 90 days
  • Used in postmenopausal atrophy of the vagina
48
Q

Vaginal Administration (Pessary) - Local Delivery

  • E.. 10 μg vaginal tablets (inserts) (Vagifem)
A
  • Estradiol 10 μg vaginal tablets (inserts) (Vagifem)​
49
Q

Intra-uterine Progestogen-only device - Local delivery

  • … Intrauterine system (IUS) (Mirena, Jaydess, Levosert) levonorgestrel (52 mg) released into uterine cavity over … or … years
A
  • Contraceptive Intrauterine system (IUS) (Mirena, Jaydess, Levosert) levonorgestrel (52 mg) released into uterine cavity over 3 or 5 years
50
Q

Release of LNG from different dosage forms

A
  • The levonorgestrel (LNg) intrauterine device (IUD) releases small amounts of levonorgestrel, a form of progesterone, into the uterus each day.
51
Q

Eicosanoid hormones - Local delivery

  • Prostaglandin E2 (Prostin E2, dinoprostone)
  • … gel (Primigyn)
  • Vaginal …/… (Propess)
    • PGE2 released over … hours, local action to ripen the cervix
A
  • Prostaglandin E2 (Prostin E2, dinoprostone)
  • Vaginal gel (Primigyn)
  • Vaginal pessary/tablet (Propess)
    • PGE2 released over 12 hours, local action to ripen the cervix

Year 2 Medicine (162 decks)

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