Topic 4: Peripheral Pain, Inflammation, Dermatology Flashcards

1
Q

Erythroxylum Coca

A

Common name: Cocaine
Geography: Andes in S. America
Ethnomedical Use: leaves are chewed with alkaline substance by Quechua people today (Incan people in the past)
Active compounds: Cocaine Alkaloid
Chemical derivatives: Procaine HCl, tetracaine, lidocaine, tocainide & procainamide

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2
Q

Cocaine Mechanism of Action as an Analgesic

A

inhibition of local norepinephrine reuptake.
Causes local vasoconstriction
Local anesthetic by blocking nerve impulses

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3
Q

Tetracaine Mech of Action & Use

A

local anesthetic –> nerve impulse blockage (long duration action)

Used topically as an anesthetic for cornea of the eye

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4
Q

Procaine HCl Mechanism of Action & Use

A

local anesthetic –> nerve impulse blockage (short duration of action)

Used as an infiltrative anesthetic by dentists

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5
Q

Lidocaine mechanism of action & Use

A

local anesthetic –> nerve impulse blockage (intermediate duration of action)
Blocks both open and inactivated cardiac Na+ channels–> slows conduction of heart

Used as a local anesthetic by dentists and to suture lacerations. Also used to treat ventricular arrhythmias

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6
Q

Tocainide & procainamide mechanism of action

A

blocks both open and inactivated cardiac Na+ channels –> slows conduction of heart

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7
Q

Cocaine Therapeutic Uses

A

applied topically by dentists and nose and throat experts

  • local anesthetic
  • local vasoconstrictor that shrinks mucosal cells
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8
Q

Filipendula ulmaria

A

Common name: meadowsweet
Geography: Eurasia , small tree in meadows & swamps
Ethnomedical Use: bark used for inflammation, pain, fever
Chemical Class: glycoside
Chemical derivatives: salicylic acid –> ASPIRIN

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9
Q

Salicin (Salix)

A

Salix alba
Common name: willow
Geography: Mediterranean Europe
Ethnomedical Use: bark used as an analagesic for headaches, antiinflammatory and fever
Active compounds: salicin (metabolizes into salicyclic acid)
Chemical derivatives: saligenin (analgesic)

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10
Q

Aspirin Mechanism of Action

A

blocks cyclooxygenase (prostaglandin synthase) which:

  • decreased the conversion of arachidonic acid to endoperoxide which:
  • decreases the formation of thromboxane A2
  • decreases prostaglandin synthesis/inflammation &inhibits platelet hemostasis (makes them less sticky)
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11
Q

COX-1 Enzyme

A

cyclooxygenase
-enzyme involved in prostaglandin synthesis
makes prostaglandins that are responsible for maintenance and protection of the GI tract
-blocked by aspirin

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12
Q

COX-2 Enzyme

A

cyclooxygenase

  • enzyme involved in prostaglandin synthesis
  • makes prostaglandins that are responsible for inflammation and pain.
  • blocked by aspirin
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13
Q

COX-2 selective inhibition

A

COX 2 selective inhibitor is a form of a non-steroidal anti-inflammatory drug (NSAID). It selectively targets COX-2. Provides pain relief without irritating the stomach lining.

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14
Q

Aspirin and COX enzymes

A

inhibits both (equipotent).

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15
Q

Ibuprofen and COX enzymes

A

has a 7x greater inhibition of COX-2 in comparison to COX-1

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16
Q

Aspirin Therapeutic Uses

A
taken orally
analgesic
anti inflammatory
antipyretic (fever)
antiplatelet
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17
Q

Salicyclic acid, salicin, & saligenin Topical therapeutic uses

A

Salicyclic acid:

  • warts, acne, eczema
  • pain caused by: rheumatism, myalgia, nerualgia, headaches

salicin: antiheumatic (joint pain/inflammation)
saligenin: applied topically as analgesic

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18
Q

Disogenin

A

Dioscorea Mexicana
Common name: wild yam
Geography: Mexico
Ethnomedical Use:anti inflammatory, fish poisons
Active compounds: diosogenin
Chemical Class:steroid
Chemical derivatives: precursor to glucocorticoids

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19
Q

Glucocorticoids/corticosteroids

A
hydrocortisone
cortisone
prednisone
prednisolone
methylpredisolone
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20
Q

Glucocorticoid Mechanism of Action

A

Down regulates cytokine production which reduces inflammation:
- steroid binding to glucocorticoid receptor (GR) in cell cytoplasm results in activation of receptor and translocation to the nucleus where regulatory regions of certain genes are effected including negative regulation for genes that code for cytokines

Reduces prostaglandin production which reduces inflammation:
-blocks the conversion of phospholipid to arachidonic acid which blocks the formation of protasglandins.

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21
Q

Antiinflammatory uses of glucocorticoids

A

skin: eczema, dermatitis, psoriasis
eye: conjunctivitis
joint: arthritis
GI: Inflammatory bowel disease
Respiratory: asthma
Kidney: nepthrotic syndrom

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22
Q

Hydroxychoroquine (Cinchona officinalis)

A

Geography: S. American rainforest

Ethnomedical Use: bark used for rheumatoid arthritis and lupus:

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23
Q

Colchicum autumnale

A

Common name: crocus
Geography: Europe & N. America, gardens
Ethnomedical Use: corms used for gout, arthritis,inflammation and pain.
Used today for all of the above and autoimmune arthritis & lupus

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24
Q

Colchicum Mech of Action

A

causes a doubling of chromosomes by disorganizing the spindle mechanism at mitosis

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25
Harpagophytum procumbens
Common name: devil's claw Geography: Southern Africa, Kalahari desert Ethnomedical Use: root used for lower back, hip, and knee pain Active compounds: harpagoside anti inflammatory
26
Cold and Hot pain receptors
Menthol- cold capsaicin- heat wasabi- heat
27
TRPM8
cold sensitive ion channel associated with the menthol pain receptor
28
TRVP1
heat sensitive ion channel associated with capsaicin pain receptor
29
TRPA-1
heat sensitive ion channel associated with wasabi pain receptor.
30
Wasabi receptors
contains, TRPA-1, an ion channel in sensory nerves under the skin, including mouth and mucus membranes. Detect temperature, mechanical abrasion and irritating chemicals.
31
Activators of Wasabi Pain receptor (TRPA-1)
``` wasabi -enhancer horse radish- enhancer hot mustard - enhancer onion - enhancer garlic- enhancer cholorquine endogenous mast cell, BAM8-22, which is released during inflammation ``` All contain allyl isothiocynate
32
Wasabi
``` Eutrema Wasabi Common name: wasabi Geography: Japan Ethnomedical Use: condiment Active compounds: allyl isothiocyanate, stimulates TRPA-1; wasabi pain receptor ```
33
Horse Radish (Amoracia rusticana)
Geography: S.E. Europe and W. Asia Ethnomedical Use: condiment Active compounds: allyl isothiocyanate, stimulates TRPA-1, wasabi pain receptor
34
Mustard (Brassica)
Geography: Asia Ethnomedical Use: condiment Active compounds: isothiocyanates, stimulate wasbi hot receptors Brassica Nigra: black mustar Brassica Juncea: Brown/Indian mustard Brassica hirta: white/yellow
35
Onion (allium cepa)
Geography: Central Asia Ethnomedical Use: food, spice, condiment Active compounds:allyl isothiocyanate, stimulates wasabi pain receptors
36
Onion lacrymatory factor
when an onion is cut, cells are broken releasing alliinases to break down amino acid sulphenis acids which are converted into syn-propanethial-S-oxide, a volatile gas known as the onion lacrymatory factor (LF)
37
Garlic (allium sativum)
Geography: Asia Ethnomedical Use: food, spice, condiment Active compounds:ally isothiocyanate, stimulates wasabi pain receptors
38
Molecules that induce itching by way of wasabi receptor
Cholorquine, BAM8-22, Mucuna prureins
39
Cholorquine Mechanism as a pain/itch molecule
stimulates wasabi pain receptor, TRPA-1. It also stimulates MrgprC11 itch receptor. Cholorquine first binds to the wasabi receptor and opens the ion channel, depolarizing the nerve cell which then sends an itch signal to the brain.
40
BAM8-22
endogenous peptide released during inflammation by immune cells (mast cells). Stimulates the wasabi receptor & the MrgprC11 itch receptor. It first stimulates the wasabi receptor opening to ion channels and sends an itch signal to the brain
41
Capsaicin Heat Receptor
Heat sensitive. | TRVP1 is the ion channel associated with this receptor.
42
Capsicum
capsicum annuum- chile pepper capicum frutescents- tabasco pepper Geography: Tropical America Ethnomedical Use: topically used as an analgesic for: arthritis, inflammation, neuralgia orally used as a: stimulant, antimicrobial Active compounds: capsicin
43
Capsaicin Mechanism of action
The capsaicin receptor is a heat activated ion channel in the pain pathway. Noxious temperature receptors are sensitive to capsaicin. These receptors get excited and result in pain perception. prolonged perception causes the receptors to become desensitized to the capsaicin and other noxious stimuli.. -potent depletor of the neurotransmitter substance P103
44
Capsaicin therapeutic uses today
pain in skin, muscles, joints ,rheumatism, & neuralgia | pruristis (itching) caused by psoriasis or other skin disorders
45
Cloves (syzygium aromaticum)
Geography: Asia Ethnomedical Use: oil is used topically on skin as analgesic and is applied topically to gums to treat toothaches stimulates heat sensitive receptors
46
Zingiber Officinalis (ginger)
Common name: ginger Geography: Asia Ethnomedical Use: analgesic, digestive, anti-nausea, flavoring, antipyretic, antibacterial properties. Can also induce salivation Active compounds: non volatile phenylpropanoid derived compounds (gingerols & shogaols). Contribute to pungent taste hot varieties enhance heat sensitive receptors
47
Piper Nigrum (Black Pepper)
Common name: Pepper Geography: India Ethnomedical Use: spice Active compounds:peperine, which may enhance heat receptors
48
Cold Sensitive Receptors
Menthol Pain receptor which is associated with the ion channel TRPM8.
49
Molecules that stimulate cold sensitive receptors
peppermint camphor eucalyptus
50
TRPM8 Mechanism
When TRPM8 is activated there is an initial sense of cold which is followed by desensitization and analgesia.
51
Mentol Piperita
Common name: peppermint Geography: Europe Active compounds:menthol stimulates menthol pain receptor (cold) and TRPM8
52
Cinnamomum camphora
Geography: Asia Active compounds:camphora (leaves) stimulates menthol pain receptor and TRPM8
53
Eucalyptus globulus
Common name: Eucalyptus Geography:Australia Ethnomedical Use: Topically as analgesic Phytomedicines: oil, cineole (eucalyptol) is 70% of the oil.
54
Acmella Oleraceae (toothache plant)
Geography: South America Ethnomedical Use: leaves consumed as a salad vegetable. Used to treat tooth pain, tongue pain, & sore throats. Also helps induce salivation Active compounds: spilanthol- makes a tingling sensation on the tongue Chemical Class: Chemical derivatives:
55
Wintergreen Oil
Contains Gaultheria procumbens (wintergreen) and Betula Lenta (sweet birch)
56
Gaultheria procumbems (wintergreen) & Betula Lenta (Sweet Birch)
Geography: Eastern USA Active compounds: methyl salicylate They block the production of prostaglandins by blocking cyclooxygenases (prostaglandin synthase) which inhibits conversion of arachidonic acid to endoperoxide. Acts as an anti-inflammatory
57
Tiger Balm
topical analgesic.with ingredients that have heat and cold sensitive analgesic effects.
58
Aloe Vera
Common name: aloe Geography: Aloe Vera- S.W. Arabia Ethnomedical Use: applied topically to treat burns and skin infections
59
Hamamelis virginiana (witch Hazel)
Geography: Easter North America Mechanism of action: vasoconstriction and astringent effects ``` Used to topically for: bruises hemorrhoids varicose veins aftershave ```
60
Arnica (Arnica montana & arnica fulgans)
``` Geography: montana- N. &C. Europe, fulgans: N. America Therapeutic uses: applied topically for -skin inflammation -bruises -blunt injuries -Rheumatism ```
61
Calendula Officinalis
``` Common name: Marigold, calendula Geography:Mediterranean Area Therapeutic Uses: topical application for -skin inflammation -skin infections -wound healing ```
62
Avena Sativa (oats)
Europe | used as topical applicant for skin itching
63
Berberis aquafolium
NW USA Common name: oregon Berry Bark and root used Used to treat psoriasis
64
Hypericum Perforatum
``` St. John's Wort Eurasia, naturalized in N. America active compounds: hyperforin (antidepressant, antidiabetic), hypericin (wound healing) Taken orally for: depression Type II diabetes Topically for: wound healing ```
65
Carica Papaya
Common Name: papaya Geography: Tropical Americ Active Molecules: protease enzymes papain, chymopapain A &B from papaya fruit Mechanism of Action: these enzymes help digest protein and debride necrotic wound tissue and enhance wound healing. Also helps with digestion
66
Bromelain (Ananas Comosus)
Common name: pineapple, ananas (tupi name) Geography: S. America Cultural Origins: Tupi Indians in S. America Active Molecules: protease enzyme bromelain (from stem)
67
Pineapple Mechanism of action
The protease enzyme help enzymatically digest protein and debride necrotic wound tissue and enhance wound healing.
68
Pineapple Therapeutic uses
applied topically to debride necrotic tissue and enhance wound healing. taken orally to treat diarrhea and enhance digestion