Topic 4: Peripheral Pain, Inflammation, Dermatology Flashcards
Erythroxylum Coca
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
Cocaine Mechanism of Action as an Analgesic
inhibition of local norepinephrine reuptake.
Causes local vasoconstriction
Local anesthetic by blocking nerve impulses
Tetracaine Mech of Action & Use
local anesthetic –> nerve impulse blockage (long duration action)
Used topically as an anesthetic for cornea of the eye
Procaine HCl Mechanism of Action & Use
local anesthetic –> nerve impulse blockage (short duration of action)
Used as an infiltrative anesthetic by dentists
Lidocaine mechanism of action & Use
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
Tocainide & procainamide mechanism of action
blocks both open and inactivated cardiac Na+ channels –> slows conduction of heart
Cocaine Therapeutic Uses
applied topically by dentists and nose and throat experts
- local anesthetic
- local vasoconstrictor that shrinks mucosal cells
Filipendula ulmaria
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
Salicin (Salix)
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)
Aspirin Mechanism of Action
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)
COX-1 Enzyme
cyclooxygenase
-enzyme involved in prostaglandin synthesis
makes prostaglandins that are responsible for maintenance and protection of the GI tract
-blocked by aspirin
COX-2 Enzyme
cyclooxygenase
- enzyme involved in prostaglandin synthesis
- makes prostaglandins that are responsible for inflammation and pain.
- blocked by aspirin
COX-2 selective inhibition
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.
Aspirin and COX enzymes
inhibits both (equipotent).
Ibuprofen and COX enzymes
has a 7x greater inhibition of COX-2 in comparison to COX-1
Aspirin Therapeutic Uses
taken orally analgesic anti inflammatory antipyretic (fever) antiplatelet
Salicyclic acid, salicin, & saligenin Topical therapeutic uses
Salicyclic acid:
- warts, acne, eczema
- pain caused by: rheumatism, myalgia, nerualgia, headaches
salicin: antiheumatic (joint pain/inflammation)
saligenin: applied topically as analgesic
Disogenin
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
Glucocorticoids/corticosteroids
hydrocortisone cortisone prednisone prednisolone methylpredisolone
Glucocorticoid Mechanism of Action
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.
Antiinflammatory uses of glucocorticoids
skin: eczema, dermatitis, psoriasis
eye: conjunctivitis
joint: arthritis
GI: Inflammatory bowel disease
Respiratory: asthma
Kidney: nepthrotic syndrom
Hydroxychoroquine (Cinchona officinalis)
Geography: S. American rainforest
Ethnomedical Use: bark used for rheumatoid arthritis and lupus:
Colchicum autumnale
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
Colchicum Mech of Action
causes a doubling of chromosomes by disorganizing the spindle mechanism at mitosis
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
Cold and Hot pain receptors
Menthol- cold
capsaicin- heat
wasabi- heat
TRPM8
cold sensitive ion channel associated with the menthol pain receptor