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Question

what also can effect the distribution of drugs? (for unbound drugs)

Answer 1

* *unbound:** - capillary structure (blood brain barrier) - chemical nature of drug - blood flow through tissues (hydrophobic drugs0 - presences of non active binding drugs

Answer 2

- ligand gated ion channel: GABA_A receptor - g-protein coupled receptors: B-adrenoreceptor - kinase-linked receptors (like tyrosine): VEGF receptor - nuclear receptors: Oestrogen receptor

Answer 3

1. steriod hormones 2. thryoid hormones 3. retinoids 4. vitamin D ## Footnote **all hydrophobic signal molecules** (hydrophilic drugs cant pass through cell membrane) **work by:** a) activating nuclear receptors: can bind to DNA regions b) regulate gene transcription

Answer 4

. **tachyphylaxis**: acute tolerance from rapid and repeated admin of drugs in short intervals (the image) 2. **tolerance**: chronic longer term admin can reduce drug effect (e.g. alchohol) **mechanisms for tolerance or tachyphylaxis:** 1. receptor _desensitized_ or loss of receptors 2. receptor _internalisation_ (degraded in lysosome) 3. increased _metaboloic degradation of drug_

Answer 5

**via process of B Arrestin mediated internalisation:** - B-arrestin binds to gcpr - B-arrestin desensitised - B-arrestin internalised - B-arrestin recyled OR -B-arrestin degraded

Answer 6

B-arrestin

Answer 7

intrathecal (into CSF )

Answer 8

**cytochrome P450 family enzymes**

Answer 9

if goes back via **bile**: - goes back into GI system: i) **phase 1 drug:** reabsorbed from GI system and goes back to liver 4 further met. ii) **phase 2 drug:** exits via defecation

Answer 10

clearance: rate of elimination in relation to the drug concentration ## Footnote **clearance = rate of elimination (through urine) / concentration remaining (in blood plasma)**

Answer 11

* *loading dose:** - larger than normal dose - gets to therapeutic range quicker (emergencies) - mainly for drugs with large vol. of distribution * *maintenance dose:** - small fixed dose - maintains drug in therapeutic range

Answer 12

- **NANC = non-adrenergic non cholinergic neurons** (NTs aren't adreneric or cholinergic class) - location: peripheral tissues - smooth muscle in GI, airways and reproductive tracts - NTs: nitric oxide, ATP, 5HTP, neuropeptide Y

Answer 13

**- pentameric sodium ion channel** * *- 2 alpha subunits:** - alpha 3 found on autonomic ganglia - alpha 1 found on neuromuscular junction - alpha 4 & 7 found in CNS **- 3 beta subuits**

Answer 14

- work at both **nicotinic and muscarinic receptors**: have an effect on both para and sympathetic NS - carbachol: treats **glaucoma**

Answer 15

5 types: - M1 = excitatory: 2nd messenger = IP3 & DAG - M2 = inhibitory: 2nd messenger = cAMP - M3 = excitatory: 2nd messenger = IP3 & DAG - M4 and M5 in CNS (dont need to know)

Answer 16

botulinium toxin (botox) - prevents ACh release: stops synapse signalling - irreversble - can be used for XS sweating, overactive bladder or muscle spasms

Answer 17

produces a similar response as **noradrenaline and adrenaline** on the sympathetic NS classes: * *i) monoamines ii) catecholamines (e.g. noradrenaline, adrenoline)**

Answer 18

GCPR - can have excitatory or inhibitory response (depending on 2nd messenger system)

Answer 19

- stimulate GI function - cognitive enhancers (given to AD patients) - skeletal muscle activity

Answer 20

* *alpha**: - alpha 1: _postsynaptic_ excitatory - alpha 2: _presynaptic_. inhbits further release of noradrenaline * *beta**: - beta 1: _postsynaptic_ excitatory - beta 2: _postsynaptic_ excitatory - beta 3: _postsynaptic_ excitatory

Answer 21

M3: * *i) eye:** - pilocarpine: pupil constrict (agonist) - tropicamide: pupil dilates (antagonist) * *ii) lungs:** - ipatroprium: lungs conflate (antagonist) * *iii) gut:** - neostgimine: gut more moveable (antagonist) - scopolamine: inhibits peristalsis - antispasmodic (agonist)

Answer 22

- prescribed as sedative or hypnotic: - **S-thalidamide** = **effective sedative** * *- R-thalidamide** = **teratogenic** (an agent that can disturb the development of the embryo or fetus) both given - made disformities

Answer 23

▪ **Collagens**: Major protein of the body (25%) and The ECM ▪**Elastin**: Provides elasticity and resilience to tissues such as the arteries, lungs, tendons, skin, and ligaments ▪**Glycoproteins**: Molecules made up of proteins and carbohydrates e.g., laminin and fibronectin Found on the surface of the lipid bilayer of cell membranes (cell surface) ▪**Proteoglycans:** Molecules made up of a core protein attached to glycosaminoglycans (GAGs) Found in connective tissues

Answer 24

it is a adhesion protein, found in lipid bilayer of cells. helps to hold up the cell on the ECM

Answer 25

found in **cytoplasm**, part of cytoskeleton: 1. cause the cell to be held in place 2. structural support

Answer 26

1. embryo development 2. cancer development

Answer 27

Triple helical structure formed by 3 peptide chains : ▪every 3rd amino acid is glycine ▪Gly-X-Y (proline-hydroxyproline)

Answer 28

too much ECM - assocaited with chronic disease **fibrosis:** too much ECM - becomes tough

Answer 29

* *non-fibrillar collagen:** * *-**forms microfibrils or mesh-like structures. - therefore is used for anchorage of cells and filtration - major structural components of basement membranes - relatively thin layers of ECM * *fibrillar collagen:** - forms well-organised banded fibrils, with provide high tensile strength. therefore is used for major components in tendons, ligaments, skin etc

Answer 30

_brittle bone disorder_ **in type 1 collagen:** single base mutations cause Gly to convert to bulky amino acid. this prevents the corrected triple helix formation of collagen into fibrils. therefore is loose triple helix

Answer 31

* *Type 1:** a) autosomal dominant b) most common - 50% of cases c) mildest type d) COL1A1 & A2 genes are mutated on chr. 17 and 7 respectively. causes an amino acid change - looser collagen chain and looser triple helix. * *Type 2:** - more severe - babies born with so many broken bones they die. - usually new mutation - dominant if affected individuals survive

Answer 32

- **rich in glycine and proline** - like collagen, but has more **valine** which interacts with hydrophobic domains, therefore makes it elastic. - elastin fibres are normally covered by the glycoprotein **fibrillin.** - can stretch in 2D. - when in relaxed state, fibres are jumbled. when stretch - stretches out and gives flex.

Answer 33

-rare genetic disease (1/10000) **- fibrillin protein is mutated and usually absent:** characteristics: **tall stature, long arms and legs, arachnodactyly (spider fingers), loose joints, floppy cardiac valves, eye problems, aortic aneurysms**

Answer 34

receptors of cell surfaces for: - bacteria, viruses and toxins. START immune response hormones strength and support to ECM slime layer of bacteria and flagella

Answer 35

**both glycoproteins** _**1.** laminin:_ - cell adhesion to the ECM. - cell migration - cytoskeleton organisation _2. fibronectin_ cell adhesion to the ECM. cell migration cell shape cell differentiation cytoskeleton organisation

Answer 36

* *_proteoglycans:_** - Proteoglycans form large aggregates within tissues made up of lots of side chains of negatively charged GAGs - peptide chain with covalently bound sugars. - mainly made of GAGs (glycosaminoglycans) - 95% carb, 5% protein - GAG side chains have sulphate group - gives a negative charge. **this attracts water and so water moves into ECM** - gel forming components of ECM. **_with age:_** decrease with age - shorter core and fewer side chains - **draw and hold less water in tissue** - more likely to be damaged e.g. in vertebral discs lose water - THIS IS WHY YOU GET SMALLER IN AGE * *_with healing:_** - They are upregulated in damaged areas - They cause oedema associated with the original injury - They provide nutrients and growth

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